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Recently, there has been increased microbial and multidrug resistance in clinical field that negatively affects health because it leads to a variety of diseases due to inefficient mode of action as...

A new series of 5-chloroindoline-2,3-dione (isatin) derived ligands (L1 )-(L4 ) were prepared by reacting isatin with various diamines such as ethane-1,2-diamine, propane-1,3-diamine, butane-1,4-diamine, and benzene-1,2-diamine in an equimolar ratio to give 3-[(2-aminoethyl)imino]-5-chloro-1,3-dihydro-2H-indol-2-one (L1 ), 3-[(3-aminopropyl) imino]-5-chloro-1,3-dihydro-2H-indol-2-one (L2 ), 3-[(4-aminobutyl)imino]-5-chloro-1,3-dihydro-2H-indol-2-one (L3 ) and 3-[(2-aminophenyl)imino]-5-chloro-1,3-dihydro-2H-indol-2-one (L4 ). All ligands acted as tridentate possessing three active sites, isatin-O, azomethine-N, and amino-N for binding with the metal atoms. The structures of the isatin based Schiff bases were elucidated through their spectral (infrared, ultraviolet, nuclear magnetic resonance, and mass spectra), physical (melting point and solubility) and analytical (C, N, H %) data. The prepared ligands were reacted with Co(II), Ni(II), Cu(II), and Zn(II) transition metals in 1:2 molar ratio (metal:ligand) to form their complexes. IR, UV, NMR, conductance, magnetic moment, and elemental analysis was used to characterize the metal complexes. Metals based isatins were evaluated for their in-vitro antimicrobial properties against selected fungal and bacterial species. The anti-bacterial and anti-fungal results showed the metal chelates to be more biologically active than their parent uncomplexed ligands.

In the present research, novel unsymmetrically substituted triazole-derived Schiff base ligand 2-[[[5-[[1-(5-methylfuran-2-yl)ethylidene]amino]-1H-1,2,4-triazol-3-yl]imino]methyl]phenol (L) has been synthesized by the reaction of 1,2,4-triazole-3,5-diamine with 2-hydroxybenzaldehyde and with 5-methyl-2-acetylfuran in an equimolar ratio. The synthesized ligand L was characterized by physical methods (melting point, solubility, color) as well as by spectral techniques (IR, UV–Vis, 1H NMR, 13C NMR, and MS), elemental analysis, and computational studies. Computational analysis further elucidated the structure, polarity, stability, and nature of the ligand. The bivalent(II), trivalent(III), and tetravalent(IV) transition metal complexes were formed by reacting Mn(II), Fe(II), Co(II), Ni(II), Cu(II), Zn(II), and Cr(III) metals as chloride and, VO(IV) as sulfate with Schiff base ligand L in 1:2 (M:L) molar ratio. Ligand was coordinated with the metal ions, VO via benzaldehyde-O and azomethine-N and with Mn(II), Fe(II), Co(II), Ni(II), Cu(II), Zn(II), and Cr(III) via benzaldehyde-O, azomethine-N, and triazole-N. The structure of the metal complexes was deduced by IR, conductance, magnetic moments, and elemental analysis. Biological evaluation of triazole-derived Schiff base ligand and its metal complexes was carried out against bacterial strains, Escherichia coli, Staphylococcus aureus, Neisseria gonorrhea, and Pseudomonas syringae. Copper complex showed the highest inhibition against all bacterial strains as compared to the free ligand and amongst other metal complexes. In vitro antibacterial studies thus concluded that the prepared ligand showed bioactivity which was enhanced upon chelation/coordination with the metal ions.

Dysfunction of p53 and resistance to cancer drugs can arise through mutually exclusive overexpression of MDM2 or MDM4. Cisplatin-resistant cells, however, can demonstrate increased binding of both MDM2 and MDM4 to p53 but in absence of cellular overexpression. Whether MDM2 inhibitors alone can activate p53 in these resistant cells was investigated with the goal to establish the mechanism for potential synergy with cisplatin. Thus, growth inhibition by individual drugs and combinations was assessed by a colorimetric assay. Drug-treated parental A2780 and resistant tumor cells were also examined for protein expression using immunoblot and reverse phase protein array (RPPA) and then subjected to Ingenuity Pathway Analysis (IPA). Gene expression was assessed by real-time polymerase chain reaction, DNA damage by confocal microscopy, cell cycle by flow cytometry, and homologous recombination (HR) by a GFP reporter assay. Our results demonstrate that Nutlin-3 but not RITA (reactivation of p53 and induction of tumor cell apoptosis) effectively disrupted the p53-MDM2-MDM4 complex to activate p53, which increased robustly with cisplatin/Nutlin-3 combination and enhanced antitumor effects more than either agent alone. RPPA, IPA, and confocal microscopy provided evidence for an "apparent" increase in DNA damage resulting from HR inhibition by cisplatin/Nutlin-3. Molecularly, the specific HR protein Rad51 was severely downregulated by the combination via two mechanisms: p53-dependent transrepression and p53/MDM2-mediated proteasomal degradation. In conclusion, Nutlin-3 fully destabilizes the p53-MDM2-MDM4 complex and synergizes with cisplatin to intensify p53 function, which then downregulates Rad51 through a bimodal mechanism. As a result, HR is inhibited and antitumor activity enhanced in otherwise HR-proficient sensitive and resistant tumor cells. SIGNIFICANCE STATEMENT: Rad51 downregulation by the combination of cisplatin and Nutlin-3 inhibits homologous recombination (HR), which leads to persistence in DNA damage but not an increase. Thus, inhibition of HR enhances antitumor activity in otherwise HR-proficient sensitive and resistant tumor cells.

Described here is the development of gadolinium(III) texaphyrin-platinum(IV) conjugates capable of overcoming platinum resistance by 1) localizing to solid tumors, 2) promoting enhanced cancer cell uptake, and 3) reactivating p53 in platinum-resistant models. Side by side comparative studies of these Pt(IV) conjugates to clinically approved platinum(II) agents and previously reported platinum(II)-texaphyrin conjugates demonstrate that the present Pt(IV) conjugates are more stable against hydrolysis and nucleophilic attack. Moreover, they display high potent antiproliferative activity in vitro against human and mouse cell cancer lines. Relative to the current platinum clinical standard of care (SOC), a lead Gd(III) texaphyrin-Pt(IV) prodrug conjugate emerging from this development effort was found to be more efficacious in subcutaneous (s.c.) mouse models involving both cell-derived xenografts and platinum-resistant patient-derived xenografts. Comparative pathology studies in mice treated with equimolar doses of the lead Gd texaphyrin-Pt(IV) conjugate or the US Food and Drug Administration (FDA)-approved agent oxaliplatin revealed that the conjugate was better tolerated. Specifically, the lead could be dosed at more than three times (i.e., 70 mg/kg per dose) the tolerable dose of oxaliplatin (i.e., 4 to 6 mg/kg per dose depending on the animal model) with little to no observable adverse effects. A combination of tumor localization, redox cycling, and reversible protein binding is invoked to explain the relatively increased tolerability and enhanced anticancer activity seen in vivo. On the basis of the present studies, we conclude that metallotexaphyrin-Pt conjugates may have substantial clinical potential as antitumor agents.

PURPOSE: Oxaliplatin and satraplatin demonstrate activity against cisplatin-resistant tumor cells. Although the two platinum analogs are structurally-related, oxaliplatin is more active. Therefore, studies focusing on protein expression profiling were undertaken to identify the molecular mechanism for the difference in antitumor activity. METHODS: We included cisplatin as reference and DAP as a Pt(IV)-prodrug of oxaliplatin to offset Pt(IV) status of satraplatin, and utilized A2780, cisplatin-resistant 2780CP/Cl-16, U2OS and HCT-116 tumor cells in the investigation. Protein expressions following drug exposures were examined by Reverse Phase Protein Array and Ingenuity Pathway Analysis. Cell cycle was assessed by flow cytometry, cytotoxicity by growth inhibition assay and homologous recombination (HR) by a GFP reporter assay. RESULTS: Clustering analysis paired oxaliplatin with DAP and, surprisingly, satraplatin with cisplatin. This correlated with differential upregulation of p53/p21 pathway, with S and G2/M arrests by cisplatin and satraplatin in contrast to G1 arrest by oxaliplatin and DAP. Moreover, Rad51 and BRCA1 were severely downregulated by oxaliplatin and DAP, but not cisplatin and satraplatin. As a result, HR was inhibited only by oxaliplatin and DAP and this also contributed to their greater drug activity over cisplatin and satraplatin. CONCLUSIONS: Oxaliplatin and DAP robustly activate p53 and p21, which downregulate HR proteins to enhance drug activity. More significantly, since oxaliplatin induces a BRCAness state, it may have potential against BRCA-proficient cancers. Satraplatin, on the other hand, resembled cisplatin in its protein expression profile, which indicates that small changes in chemical structure can substantially alter signal transduction pathways to modulate drug activity.

The present research work was aimed to synthesize biologically active Schiff base compound, 2-{(E)-[(3-{[(Z)-(2-hydroxyphenyl)methylidene]amino}-1H-1,2,4-triazol-5-yl)imino]methyl}phenol (L) by condensation reaction of 2-hydroxybenzaldehyde with 3,5-diamino-1,2,4-triazole. In order to evaluate the effect of metal ions on the biological properties, ligand (L) was then coordinated to the metal ions such as Fe(II), Co(II), Cu(II), Ni(II) and Zn(II). Characterization of ligand and its metal complexes was done by physical, spectral and analytical data. The synthesized compounds were screened for antioxidant, enzyme inhibition and antibacterial/antifungal activities. The screening results indicated the ligand to possess bioactivity which significantly enhanced upon chelation/coordination with the metal ions. Computational studies were also carried out on the ligand to check orbital involvement and bonding interactions. The optimized frequency, intensity and geometry of the vibrational bands of ligand (L) were obtained through density functional theory (DFT) using 6–311++G (d.p) basis sets. Molecular stability and bond strength were also studied by carrying out the natural bond orbital analysis (NBO). The calculated HOMO and LUMO energies confirmed the charge transfer in the molecule of ligand.

Biologically important triazole derived Schiff base ligand 2-[(1Z)-N-(1H-1,2,4-triazol-3-yl)- etanimidoyl]phenol (SR) is synthesized by condensation of 3-amino-1,2,4-triazole with 2-hydroxyacetophenone. The ligand forms the corresponding complexes upon reaction with salts of VO(IV), Cr(III), Mn(II), Fe(II), Co(II), Ni(II), Cu(II), and Zn(II) in 2: 1 ratio. The Schiff base ligand coordinates to the metal atoms via nitrogen atoms of azomethine and triazole, and oxygen of acetophenone. Structures of the complexes are supported by physical and spectral data. Antibacterial activity of the synthesized triazole ligand and transition metal complexes is tested against several bacterial strains: Escherichia coli, Salmonella typhi, Bacillus subtilis, Klebsiella pneumonia, and Staphylococcus aureus. The complexes demonstrate substantial antibacterial activity.

Clinical reports have highlighted the radical increase of antibiotic resistance. As a result, multidrug resistance has emerged as a serious threat to human health. Many organic compounds commonly used as drugs in the past, no longer have pure organic mode of action rather need bio-transformation or more activation. Bulk of research has shown that they need trace amount of metal ions incorporated within the chemistry of bioactive molecules for enhancement of their potentiality to fight aggressively against resistance. The deficiency of some metal ions can also be responsible for many diseases like growth retardation, pernicious anemia and heart diseases in infants. To overcome these problems, there is a need to introduce novel strategies which have new mechanism of action along with significant spectrum of biological activity, enhanced safety and efficacy. Bioinorganic compounds have played imperative role in developing the new strategy in the form of "Metal Based Drugs". In current years there have been momentous rise of interest in the application of metal based Schiff base compounds to treat various diseases which are difficult to be treated with conventional methodologies. The unique properties of metal chelates acting as an intermediate between conventional organic and inorganic compounds provided innovative opportunities in the field of pharmaceutical chemistry. In this review, we have exclusively focused on the search of metal based 1,2,4-triazole derived Schiff base compounds (synthesized, reported and reviewed in the past ten years) that possess various biological activities such as antifungal, antibacterial, antioxidant, antidiabetic, anthelmintic, anticancer, antiproliferative, cytotoxic and DNA-intercalation activity.

Purpose: OxaliTEX is a texaphyrin-platinum(IV) prodrug with the ability to deliver the oxaliplatin payload to cisplatin-resistant tumor cells and restore wild-type p53 activation. As a result, the conjugate overcomes both multifactorial mechanisms of cisplatin resistance and transport-defective mechanism of oxaliplatin resistance. In an effort to prepare for translational studies, we have explored its distribution and pharmacokinetics (PK) in mice. Experimental Procedures: Athymic male and/or female nude mice (3-4/group), with or without subcutaneously implanted (flank) HCT-116 colon xenograft, received oxaliplatin (4 mg/kg) and an equimolar (17 mg/kg) or a similar therapeutic (50 mg/kg) dose of oxaliTEX iv. After 24 hours, mice were exsanguinated under anesthesia and plasma and tissues isolated. A separate group of female mice received oxaliTEX (50 mg/kg) and blood was taken at multiple times over the next 24 hours, plasma isolated and samples denatured to prepare protein-free supernatant (PFS) representing “free” platinum. Samples were analyzed for platinum (Pt) by flameless atomic absorption spectrophotometry. Results: At equimolar doses, gross sex differences in plasma or tissue concentrations were not observed for either drug. However, plasma Pt levels with oxaliTEX (0.6-0.7 ng Pt/ml) were 7-fold greater than with oxaliplatin (0.08-0.1 ng/ml). Similarly, a 3-fold greater concentration was also noted in liver (~1.4 vs. ~0.4 ng/mg) and heart (~0.5 vs. ~0.15 ng/mg) from mice treated with the prodrug. Tissues with ≤2-fold differences between the drugs in Pt levels were testes, kidney, ovary, lung, ileum and spleen, with undetectable levels in brain. In female mice bearing HCT-116 xenografts, the general tissue distribution pattern of each drug at the therapeutic dose was unchanged and demonstrated that increasing the oxaliTEX dose resulted in proportionate increase in tissue Pt levels. Notably, tumor Pt levels were ~5-fold greater with the conjugate (oxaliTEX, 1.1 ng Pt/mg; oxaliplatin, 0.21 ng/mg). PK analysis revealed that Pt in plasma and PFS was detectable for the entire 24 hr period and decayed in a biphasic manner, with respective α-phase half-life of 0.07 and 0.2 hr and β-phase half-life of 27 and 11 hr. The AUC in plasma and PFS was 172 and 3.7 μg.hr/ml, respectively. Conclusions: Results suggest that oxaliTEX is sequestered in the plasma by protein binding, leaving low-level systemic exposure to “free” non-protein bound Pt. Since the tissue levels are greater than oxaliplatin at equimolar and/or therapeutic doses in specific organs, this suggests that the low level exposure to “free” Pt contributes to drug tolerance of normal tissues, whereas the tumor-targeting design feature contributes to greater tumor uptake that enhances antitumor effects. Funding was provided by Cancer Prevention and Research Institute of Texas Citation Format: Guangan He, Gregory Thiabaud, Kathyrin A. Shelton, Luke J. Segura, Jonathan L. Sessler, Rick A. Finch, Zahid H. Siddik, Jonathan F. Arambula. Preclinical tissue biodistribution and plasma pharmacokinetic studies with oxaliTEX, a novel platinum(IV)-based oxaliplatin prodrug [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2021; 2021 Apr 10-15 and May 17-21. Philadelphia (PA): AACR; Cancer Res 2021;81(13_Suppl):Abstract nr 1073.

Shell and tube heat exchangers are widely used for various industrial refrigeration applications. This paper summarizes previous studies performed on single tube and bundles and the correla...

Objectives of the current study were synthesis, spectral characterization and biological screening of sulfanilamide derived Schiff bases and their metal based compounds. Sulfanilamide Schiff bases (L 1 –L 3 ) were synthesized by condensation of 4-aminobenzenesulfanilamide with 1-(furan-2-yl)ethanone, 1-(thiophene-2-yl)-ethanone, and 1-acetylindoline-2,3-dione. The ligands were used for preparation of their Co(II), Ni(II), Cu(II), and Zn(II) complexes by using metals chlorides in metal: ligand (1: 2) molar ratio. All metal chelates had octahedral geometry with bidentate ligands. The ligands and their metal complexes were characterized by physical, spectral and analytical data, and screened for in-vitro antibacterial activity against six bacterial pathogens (Escherichia coli, Shigella flexneri, Pseudomonas aeruginosa, Salmonella typhi, Staphylococcus aureus, and Bacillus subtilis) and for in vitro antifungal activity against six fungal pathogens (Trichophyton longifusus, Candida albicans, Aspergillus flavus, Microsporum canis, Fusarium solani, and Candida glabrata). The results of antimicrobial studies revealed that the ligands activity was significantly increased upon chelation.

Biologically active triazole derived Schiff bases, 2-methoxy-6-[(Z)-(1H-1,2,4-triazol-3-ylimino) methyl]phenol (L 1) and 4-[(Z)-(1H-1,2,4-triazol-3-ylimino)methyl]benzene-1,3-diol (L 2) were prepared by condensing 3-amino-1,2,4-triazole with 2-hydroxy-3-methoxybenzaldehyde and 2,4-dihydroxybenzaldehyde in the 1 : 1 molar ratio. Structures of the synthesized ligands were characterized by IR, NMR and Mass spectral data. The ligands were complexed with the ions of V, Cr, Mn, Fe, Co, Ni, Cu, and Zn to form the complexes M : L in the 1 : 2 molar ratio. The synthesized Schiff bases potentially behaved as tridentate ligands and coordinated to metal ions via azomethine-N, triazole-N, and benzaldehyde-O. Structure elucidation of complexes involved IR, UV-Vis, MS, and molar conductance data. These compounds were tested for antibacterial activity against Halomonas halophila, Chromohalobacter israelensis, Chromohalobacter salexigens, Staphylococcus aureus, Halomonas salina, and Neisseria gonorrhoeae bacterial stains. Antifungal activity of the synthesized compounds was studied by using different fungal stains like Trichophyton Longifusus, Candida Albicans, Aspergillus Flavus, Microsporum Canis, Fusarium, Solani, and Candida Glabrata. All synthesized compounds displayed high antimicrobial activity against one or more strains.

A novel series of thiophene derived Schiff bases and their transition metal- [Co(II), Cu(II), Zn(II), Ni(II)] based compounds are reported. The Schiff bases act as tridentate ligands toward metal ions via azomethine-N, deprotonated-N of ammine substituents and S-atom of thienyl moiety. The synthesized ligands along with their metal complexes were screened for their in vitro antibacterial activity against six bacterial pathogens (Escherichia coli, Shigella flexneri, Pseudomonas aeruginosa, Salmonella typhi, Staphylococcus aureus and Bacillus subtilis) and for antifungal activity against six fungal pathogens (Trichophytonlongifusus, Candida albicans, Aspergillus flavus, Microsporum canis, Fusarium solani and Candida glabrata). The results of antimicrobial studies revealed the free ligands to possess potential activity which significantly increased upon chelation.

Reported here are new platinum(IV) (Pt(IV)) complexes bearing ferrocene (Fc) moieties. These systems differ from one another only by the nature of the functional group (ester vs amide) connecting the linker to the Fc subunits. This minor structural variation (one atom difference) leads to major differences in solubility, stability, and antiproliferative activity against lung (A549) cancer cells. The host-guest chemistry of these complexes was investigated in an aqueous medium in the presence of β-cyclodextrins (β-CD), either free or in the form of a covalently linked Fc-Pt-β-CD hybrid. An inclusion complex between Fc and β-CD is formed in aqueous media, presumably as a result of hydrophobic interactions involving the Fc and the inner β-CD cavity. Consequently, it proved possible to use a β-CD-based strategy to purify the Pt-Fc conjugates in this study under aqueous conditions (by means of C18 silica gel columns). The use of a β-CD adjuvant also allowed dimethyl sulfoxide (DMSO) to be avoided as an organic cosolvent in cell studies. The amide version reported here (2) proved to be more soluble, more stable, and more active than the ester analogue (11) in A549 cells. The use of a β-CD functionalized with a fluorescent probe allowed intracellular Pt-Fc localization to be visualized by confocal fluorescence microscopy.

Polyphosphoinositides (PPIns) are a family of seven lipid messengers that regulate a vast array of signalling pathways to control cell proliferation, migration, survival and differentiation. PPIns are differentially present in various sub-cellular compartments and, through the recruitment and regulation of specific proteins, are key regulators of compartment identity and function. Phosphoinositides and the enzymes that synthesise and degrade them are also present in the nuclear membrane and in nuclear membraneless compartments such as nuclear speckles. Here we discuss how PPIns in the nucleus are modulated in response to external cues and how they function to control downstream signalling. Finally we suggest a role for nuclear PPIns in liquid phase separations that are involved in the formation of membraneless compartments within the nucleus.

Platelet-derived growth factor (PDGF)-mediated signalling has emerged as one of the most extensively and deeply studied biological mechanism reported to be involved in regulation of growth and survival of different cell types. However, overwhelmingly increasing scientific evidence is also emphasizing on dysregulation of spatio-temporally controlled PDGF-induced signalling as a basis for cancer development. We partition this multi-component review into recently developing understanding of dysregulation PDGF signalling in different cancers, how PDGF receptors are quantitatively controlled by microRNAs. Moreover, we also summarize most recent advancements in therapeutic targeting of PDGFR as evidenced by preclinical studies. Better understanding of the PDGF-induced intracellular signalling in different cancers will be helpful in catalysing the transition from a segmented view of cancer biology to a conceptual continuum.

A new series of anti-bacterial and anti-fungal mono- and di-substituted triazoles (L(1))-(L(6)) have been synthesized and characterized on the basis of their physical, spectral and analytical data. The ligands (L(1))-(L(6)) on reaction with vanadyl(IV) sulphate led to the formation of vanadyl(IV) metal complexes (1)-(4). The structure of the complexes has been established on the basis of their physical, spectral and elemental analyses data. The synthesized ligands and their vanadyl(IV) complexes have been screened in vitro for anti-bacterial activity against six bacterial species such as, Escherichia coli (ATCC 25922), Shigella flexneri (ATCC 12022), Pseudomonas aeruginosa (ATCC 27853), Salmonella typhi (ATCC 14028), Staphylococcus aureus (ATCC 25923) and Bacillus subtilis (ATCC 6051) and for in vitro anti-fungal activity against six fungal strains, Trichophyton longifusus, Candida albicans, Aspergillus flavus, Microsporum canis, Fusarium solani and Candida glabrata. The screening results showed the vanadyl complexes to be more bactericidal/fungicidal against one or more bacterial/fungal species. The synthesized compounds were also subjected to brine shrimp bioassay for scrutinizing their cytotoxicity.

Extensive research within last two decades has indicated that curcumin extracted from turmeric (Curcuma longa), exhibits anticancer potential, in part through the modulation of inflammatory pathways. However, the residual antitumor activity of curcumin-free turmeric (CFT) relative to curcumin or turmeric is not well-understood. In the present study, therefore, we determined activities of these agents in both in vitro and in vivo models of human HCT-116 colorectal cancer (CRC). When examined in an in vitro antiproliferative, clonogenic or anti-inflammatory assay system, we found that curcumin was highly active whereas turmeric and CFT had relatively poor activity against CRC cells. However, when examined in vivo at an oral dose of either 100 or 500 mg/kg given to nude mice bearing CRC xenografts, all three preparations of curcumin, turmeric, and CFT similarly suppressed the growth of the xenograft. The effect of CFT on suppression of tumor growth was dose-dependent, with 500 mg/kg tending to be more effective than 100 mg/kg. Interestingly, 100 mg/kg curcumin or turmeric was found to be more effective than 500 mg/kg. When examined in vivo for the expression of biomarkers associated with cell survival (cIAP-1, Bcl-2, and survivin), proliferation (Ki-67 and cyclin D1) and metastasis (ICAM-1 and VEGF), all were down-modulated. These agents also suppressed inflammatory transcription factors (NF-κB and STAT3) in tumor cells. Overall, our results with CFT provide evidence that turmeric must contain additional bioactive compounds other than curcumin that, in contrast to curcumin, exhibit greater anticancer potential in vivo than in vitro against human CRC. Moreover, our study highlights the fact that the beneficial effects of turmeric and curcumin in humans may be more effectively realized at lower doses, whereas CFT could be given at higher doses without loss in favorable activity.

Platinum resistance is a major limitation in the treatment of advanced non-small cell lung cancer (NSCLC). We previously demonstrated that low tissue platinum concentration in NSCLC specimens was significantly associated with reduced tumor response. Furthermore, low expression of the copper transporter CTR1, a transporter of platinum uptake was associated with poor clinical outcome following platinum-based therapy in NSCLC patients. We investigated the relationship between tissue platinum concentrations and CTR1 expression in NSCLC specimens.We identified paraffin-embedded NSCLC tissue blocks of known tissue platinum concentrations from 30 patients who underwent neoadjuvant platinum-based chemotherapy at MD Anderson Cancer Center. Expression of CTR1 in tumors and normal adjacent lung specimens was determined by immunohistochemistry with adequate controls.Tissue platinum concentration significantly correlated with tumor response in 30 patients who received neoadjuvant platinum-based chemotherapy (P0.001). CTR1 was differentially expressed in NSCLC tumors. A subset of patients with undetectable CTR1 expression in their tumors had reduced platinum concentrations (P=0.058) and tumor response (P=0.016) compared to those with any level of CTR1 expression. We also observed that African Americans had significantly reduced CTR1 expression scores (P=0.001), tissue platinum concentrations (P=0.009) and tumor shrinkage (P=0.016) compared to Caucasians.To our best knowledge this is the first study investigating the function of CTR1 in clinical specimens. CTR1 expression may be necessary for therapeutic efficacy of platinum drugs, consistent with previous preclinical studies. A prospective clinical trial is necessary to develop CTR1 into a potential biomarker for platinum drugs.

In this paper we have studied the effect of cadmium concentration and N 2 laser irradiation on steady state, photosensitivity and transient photoconductivity of Cd x Se 100− x ( x =54, 34) thin films, which were prepared by thermal vacuum evaporation method. Photoconductivity measurements on the thin films are carried out at different levels of light intensities at room temperature. The current–voltage characteristic shows ohmic behavior of the films. The photosensitivity of the Cd x Se 100− x thin films is found to decrease with increase of cadmium concentration in the system, whereas it increases after irradiation with N 2 laser. Apart from this, the photocurrent follows the I ph ∝ F γ law. Also, the differential lifetimes ( τ d ) are found to increase with increase in the cadmium concentration in the Cd x Se 100− x thin films and also with increase in the laser irradiation time.

Nonlinear optical properties of 1,4-Diamino-9,10-Anthraquinone dye in solution at different concentrations are investigated by utilizing single beam Z-scan technique using a low power continuous wave laser (λ = 532 nm). The anthraquinone dye is found to exhibit self-defocusing and reverse saturable absorption behavior. Effect of concentration on nonlinear refractive index and nonlinear absorption coefficient are also studied. The nonlinear absorption coefficient (β) and nonlinear refractive index (n2) have been evaluated from the open aperture and closed aperture Z-scan data and are found to increase with increase in concentration. The order of magnitude obtained for nonlinear refractive index and nonlinear absorption coefficient are found to be 10−6 esu and 10−4 m/W, respectively. The optical limiting behavior and induced self-diffraction patterns are also observed. To have a theoretical insight of nonlinear optical properties of 1,4-Diamino-9,10-Anthraquinone, first hyperpolarizability (β) is also evaluated by using quantum chemical calculations employing DFT method using 6-311G basis set. The results obtained confirm the nonlinear optical behavior of 1,4-Diamino-9,10-Anthraquinone dye.

A series of three bioactive thiourea (carboxamide) derivatives, N-(dipropylcarbamothioyl)-thiophene-2-carboxamide (L(1)), N-(dipropylcarbamothioyl)-5-methylthiophene-2-carboxamide (L(2)) and 5-bromo-N-(dipropylcarbamothioyl)furan-2-carboxamide (L(3)) and their cobalt(II), copper(II), nickel(II) and zinc(II) complexes (1)-(12) have been synthesized and characterized by their IR,(1)H-NMR spectroscopy, mass spectrometry and elemental analysis data. The Crystal structure of one of the ligand, N-(dipropylcarbamothioyl)thiophene-2-carboxamide (L(1)) and its nickel(II) and copper(II) complexes were determined from single crystal X-ray diffraction data. All the ligands and metal(II) complexes have been subjected to in vitro antibacterial and antifungal activity against six bacterial species (Escherichia coli. Shigella flexneri. Pseudomonas aeruginosa. Salmonella typhi. Staphylococcus aureus and Bacillus subtilis) and for antifungal activity against six fungal strains (Trichophyton longifusus. Candida albicans. Aspergillus flavus. Microsporum canis. Fusarium solani and Candida glabrata). The in vitro antibacterial and antifungal bioactivity data showed the metal(II) complexes to be more potent than the parent ligands against one or more bacterial and fungal strains.

We have developed a simple, rapid, inexpensive method for the identification of fluoranthene (Flan), benz(a)anthracene (BaA), benzo(a)pyrene (BaP), benzo(k)fluoranthene (BkF), pyrene (Pyr), benz(ghi)perylene (BghiP) in suspended particulate matter in an urban environment of Delhi. Suspended particulate matter samples of 24h duration were collected on glass fiber filter papers. Polycyclic aromatic hydrocarbons (PAHs) were extracted from the filter papers using dichloromethane (DCM) and hexane with ultrasonication method. Comparison of the characteristic emission of spectra of PAHs with standard spectra indicated the degree of condensation of aromatic compounds present in investigated mixtures. It was also possible to identify some individual compounds. However, this identification could be more effective with the use of the respective values of Δλ parameter for each particular component of the mixture.

Size distribution of PM10 mass aerosols and its ionic characteristics were studied for 2 years from January 2006 to December 2007 at central Delhi by employing an 8-stage Andersen Cascade Impactor sampler. The mass of fine (PM2.5) and coarse (PM10−2.5) mode particles were integrated from particle mass determined in different stages. Average concentrations of mass PM10 and PM2.5 were observed to be 306 ± 182 and 136 ± 84 μg m−3, respectively, which are far in excess of annual averages stipulated by the Indian National Ambient Air Quality Standards (PM10: 60 μg m−3 and PM2.5: 40 μg m−3). The highest concentrations of PM10−2.5 (coarse) and PM2.5 (fine) were observed 505 ± 44 and 368 ± 61 μg m−3, respectively, during summer (June 2006) period, whereas the lower concentrations of PM10−2.5 (35 ± 9 μg m−3) and PM2.5 (29 ± 13 μg m−3) were observed during monsoon (September 2007). In summer, because of frequent dust storms, coarse particles are more dominant than fine particles during study period. However, during winter, the PM2.5 contribution became more pronounced as compared to summer probably due to enhanced emissions from anthropogenic activities, burning of biofuels/biomass and other human activities. A high ratio (0.58) of PM2.5/PM10 was observed during winter and low (0.24) during monsoon. A strong correlation between PM10 and PM2.5 (r 2 = 0.93) was observed, indicating that variation in PM10 mass is governed by the variation in PM2.5. Major cations (NH4 +, Na+, K+, Ca2+ and Mg2+) and anions (F−, Cl−, SO4 2− and NO3 −) were analyzed along with pH. Average concentrations of SO4 2− and NO3 − were observed to be 12.93 ± 0.98 and 10.33 ± 1.10 μg m−3, respectively. Significant correlation between SO4 2− and NO3 − in PM1.0 was observed indicating the major sources of secondary aerosol which may be from thermal power plants located in the southeast and incomplete combustion by vehicular exhaust. A good correlation among secondary species (NH+, NO3 − and SO4 2−) suggests that most of NH4 + is in the form of ammonium sulfate and ammonium nitrate in the atmosphere. During winter, the concentration of Ca2+ was also higher; it may be due to entrainment of roadside dust particles, traffic activities and low temperature. The molar ratio (1.39) between Cl− and Na+ was observed to be close to that of seawater (1.16). The presence of higher Cl− during winter is due to western disturbances and probably local emission of Cl− due to fabric bleaching activity in a number of export garment factories in the proximity of the sampling site.

The use of carbon dioxide and ammonia in low temperature cascade systems is gaining momentum in the industrial refrigeration market. The use of a plate exchanger as cascade condenser is a viable option due to the high thermal efficiency and smaller footprint characteristics of such exchangers. There is a lack of reliable data in the open literature on condensation of carbon dioxide and evaporation of ammonia in such heat exchangers. This article presents the latest research on condensation of carbon dioxide and evaporation of ammonia in various corrugated plate exchangers at different saturation temperature and heat/mass flux. The data are reduced to generalized empirical correlations to be used as design tools by engineers. It also discusses the mechanical aspects of plate exchanges and their suitability in cascade systems.

Water-soluble platinum(IV) prodrugs, which proved kinetically stable to reduction in the presence of physiological concentration of ascorbate, were quickly reduced to their active form, oxaliplatin, when co-incubated with a macrocycle metallotexaphyrin (i.e., Motexafin Gadolinium (MGd)). The reduction of Pt(IV) to Pt(II) promoted by MGd occurs in cell culture as well, leading to an increase in the antiproliferative activity of the Pt(IV) species in question. The mediated effect is proportional to the concentration of MGd and gives rise to an enhancement when the prodrug is relatively hydrophilic. MGd is known to localize/accumulate preferentially in tumor tissues. Thus, the present "activation by reduction" approach may allow for the cancer-selective enhancement in the cytotoxicity of Pt(IV) prodrugs.

A new series of compounds derived from thiophene-2-carboxamide were synthesized and characterized by IR, 1H-NMR and 13C-NMR, mass spectrometry and elemental analysis. These compounds were further used to prepare their Co(II), Ni(II), Cu(II) and Zn(II) metal complexes. All metal(II) complexes were air and moisture stable. Physical, spectral and analytical data have shown the Ni(II) and Cu(II) complexes to exhibit distorted square-planar and Co(II) and Zn(II) complexes tetrahedral geometries. The ligand (L1) and its Cu(II) complex were characterized by the single-crystal X-ray diffraction method. All the ligands and their metal(II) complexes were screened for their in-vitro antimicrobial activity. The antibacterial and antifungal bioactivity data showed that the metal(II) complexes were found to be more potent than the parent ligands against one or more bacterial and fungal strains.

A newly synthesised series of antibacterial and antifungal triazole-derived Schiff base ligands (L 1 )–(L 5 ) has been prepared by the condensation reaction of 3,5-diamino-1,2,4-triazole with methyl-, chloro- and nitro-substituted thiophene-2-carboxaldehydes in (1:2) molar ratio. The most probable structures of the synthesised Schiff base ligands were established on the basis of their physical, spectral (IR, 1H and 13C NMR and mass spectrometry) and analytical (CHN analysis) data. These Schiff bases potentially act as bidentate ligand and were further made to react with the vanadyl(IV) sulphate (VOSO4·5H2O) in (1:2) (metal:ligand) molar ratio to prepare their oxovanadium(IV) complexes (1)–(5). All oxovanadium(IV) complexes showed a square-pyramidal geometry which was established on the basis of their physical, spectral and analytical data. The Schiff base ligands and their vanadyl(IV) complexes have been screened for their in vitro antibacterial, antifungal and brine shrimp bioassay. The antimicrobial activity data showed the vanadyl(IV) complexes to be more potent antibacterial and antifungal than the parent Schiff bases against one or more bacterial and fungal species.

A series of new triazoles and their oxovanadium(IV) complexes have been synthesized, characterized and evaluated for antibacterial/antifungal properties. The new Schiff bases ligands (L(1))-(L(5)) were prepared by the condensation reaction of 3,5-diamino-1,2,4-triazole with 2-hydroxy-1-naphthaldehyde, pyrrole-2-carboxaldehyde, pyridine-2-carboxaldehyde, 2-acetyl pyridine and 2-methoxy benzaldehyde. The structures of the ligands have been established on the basis of their physical, spectral (IR, (1)H and (13)C NMR and mass spectrometry) and elemental analytical data. The prepared ligands were used to synthesize their oxovanadium(IV) complexes (1)-(5) which were also characterized by their physical, spectral and analytical data and proposed to have a square pyramidal geometry. The ligands and their complexes were screened for in vitro antibacterial activity against six bacterial species such as, Escherichia coli, Shigella flexneri, Pseudomonas aeruginosa, Salmonella typhi, Staphylococcus aureus, and Bacillus subtilis and for in vitro antifungal activity against six fungal strains, Trichophyton longifusus, Candida albicans, Aspergillus flavus, Microsporum canis, Fusarium solani, and Candida glabrata. Cytotoxic nature of the compounds was also reported using brine shrimp bioassay method against Artemia salina.

New metal based triazoles (1–12) have been synthesized by the interaction of novel Schiff base ligands (L1–L3) with the Co(II), Ni(II), Cu(II) and Zn(II) metal ions. The Schiff base ligands and their all metal(II) complexes have been thoroughly characterized using various physical, analytical and spectroscopic techniques. In vitro bacterial and fungal inhibition studies were carried out to examine the antibacterial and antifungal profile of the Schiff bases in comparison to their metal(II) complexes against two Gram-positive, four Gram-negative and six fungal strains. The bioactivity data showed the metal(II) complexes to have more potent antibacterial and antifungal activity than their uncomplexed parent Schiff bases against one or more bacterial and fungal species. Copyright © 2012 John Wiley & Sons, Ltd.

A new series of four biologically active triazole derived Schiff base ligands (L(1)-L(4)) and their cobalt(II), nickel(II), copper(II) and zinc(II) complexes (1-16) have been synthesized and characterized. The ligands were prepared by the condensation reaction of 3-amino-5-methylthio-1H-1,2,4-triazole with chloro-, bromo- and nitro-substituted 2-hydroxybenzaldehyde in an equimolar ratio. The antibacterial and antifungal bioactivity data showed the metal(II) complexes to be more potent antibacterial and antifungal than the parent Schiff bases against one or more bacterial and fungal species.

A computation model has been developed for the rational design of bioactive pharmacophore sites as anti-viral candidates based on available X-ray structures of drugs. The compounds have been previously screened for anti-viral activity against HIV-Integrase (HIV IN). Amongst the series, the most potent compounds, 4k and 4d (low μM IC50) were tested in viral cultures for their ability to present potentials (O 1 δ− –O 2 δ− –O 3 δ− ) for anti-viral pharmacophore site but represent a potential risk of toxicity. Furthermore, the compounds 4k and 4d showed potent anti-HIV IN activity. A good correlation was obtained between the theoretical predictions of bioavailability using POM suite (Petra/Osiris/Molinspiration containing Lipinski’s rule-of-five) and experimental verification. The structure–activity relationships were also analyzed to vindicate the POM results. A series of known anti-HIV agents; the amide-containing diketoacids were POM and 3D-QSAR analyzed in goal to understand and develop more potent/selective HIV IN inhibitors. Their inhibition of HIV IN was attributed to them containing O1,O2,O4-pharmacophore site. The structure–activity relationships were discussed on the basis of POM analyses.

Condensation pressure drop of carbon dioxide in brazed plate heat exchangers was investigated, and is presented in this paper. Carbon dioxide is known as an environmental friendly refrigerant with an Ozone Depletion Potential (ODP) equal to zero and Global Warming Potential (GWP) equal to unity, and has favorable thermodynamic and transport properties though it requires higher operating pressures (∼15–30 bar). Brazed-type plate heat exchangers that can withstand high pressure are a good choice for such applications. This paper presents the procedure, data collection, and results for three brazed plate heat exchangers with different inner geometries. The test exchangers showed good performance at high system pressures with reasonable pressure drops (less than 8%). The collected experimental data that covered real world operating conditions are valuable for the design of cascade condensers with carbon dioxide as the low-side refrigerant.

A method of measurement of diffusion length L in p type c-Si wafers based on the lateral collection of minority carriers is reported. In this method, wafer requires a p–p+ junction on entire back surface and an n+–p interface on a part of the front surface leaving the rest part as bare for illumination. A photo-current Isc is generated when a rectangular area of a part of the bare front surface in the vicinity of the n+–p interface is illuminated with a laser beam. The magnitude of Isc varies with the normal distance d between the electron collecting n+–p interface and the nearest edge of the illuminated region. The slope Φ of the normalized Isc vs. d curve is used to determine a parameter sinh−1θ, which has a linear relation with d. The reciprocal of the slope of sinh−1θ vs. d curve in the linear region gives the diffusion length L. The value of L is less susceptible to error due to the effect of Sf of bare silicon surface if the linear region of sinh−1θ vs. d curve lies in the region of smaller d values. The present method has an advantage over the other methods in that it does not depend on the intensity of the illumination and absorption coefficient of Si. Additionally, method has no limitation in terms of wafer thickness to diffusion length ratio and is applicable to all practical L values.

Treatment of glioblastoma (GBM) includes surgery and chemoradiation with temozolomide. Due to chemoresistance, nearly all tumors recur and 5-year survival is less than 3%. Various treatments, including anti-angiogenic treatment with bevacizumab, nitrosoureas and topoisomerase inhibitors, have failed to improve overall survival in recurrent GBM (rGBM). GBM tumors expressing O6-methylguanine-DNA-methyltransferase (MGMT) are resistant to temozolomide and nitrosourea, and deficient DNA mismatch repair (MMR) confers secondary resistance to temozolomide. Our recent phase I/II trial in rGBM patients previously treated with temozolomide and bevacizumab, suggested that VAL-083 may offer a clinically meaningful survival benefit for rGBM patients. VAL-083 is a first-in-class bi-functional DNA-targeting agent that readily crosses the blood-brain barrier and accumulates in brain tumor tissue. The mechanism-of-action of VAL-083 differs from other alkylating agents and overcomes both MGMT- and MMR-related resistance to temozolomide, in vitro. VAL-083 rapidly induces interstrand cross-links at N7-guanine, causing DNA double-strand breaks and persistent activation of the homologous recombination (HR) DNA repair pathway. Furthermore, VAL-083 potency is increased in HR-deficient cancer cells, suggesting increased cytotoxicity in HR-impaired tumors. Hypoxic GBM cells downregulate HR activity, thus proposing increased VAL-083 potency in hypoxic tumors. Bevacizumab increases intratumor hypoxia, suggesting VAL-083 as a treatment option in HR-deficient or hypoxic cancers following, or as part of combination with, bevacizumab. The potency of VAL-083 as part of a combinatory treatment with bevacizumab was investigated in GBM models under hypoxia both in vitro and in vivo. Separately, we demonstrated that VAL-083 induces irreversible S/G2-phase cell-cycle arrest, thus proposing synergy with S-phase specific chemotherapeutics, including topoisomerase and PARP inhibitors. Here, we investigated cytotoxicity of VAL-083 combinations with various topoisomerase and PARP inhibitors in a range of cancer cells. Our results support the potential of VAL-083 to i) overcome resistance to temozolomide, and ii) display synergy as part of combinatory therapies with topoisomerase or PARP inhibitors.

Biologically active triazole Schiff bases (L1L3) derived from the reaction of 3-amino-1,2,4-triazole with chloro-, bromo- and nitro- substituted salicylaldehydes and their Zn(II) complexes (1–3) have been synthesized and characterized by their physical, spectral and analytical data. Triazole Schiff bases potentially act as tridentate ligands and coordinate with the Zn(II) metal atom through salicylidene-O, azomethine-N and triazole-N. The complexes have the general formula [M(L-H)2], where M = zinc(II) and L = (L1–L3), and observe an octahedral geometry. The Schiff bases and their Zn(II) complexes have been screened for in-vitro antibacterial, antifungal and brine shrimp bioassay. The biological activity data show the Zn(II) complexes to be more potent antibacterial and antifungal than the parent simple Schiff bases. Copyright © 2011 John Wiley & Sons, Ltd.

Various novel barbituric and thiobarbituric acid derived sulphonamides were synthesized in excellent yield via three components single pot reaction; and these were screened for in vitro urease inhibition studies against jack bean urease. The compounds 1-7 were found to exhibit a low to moderate activity whereas compounds 8-14 showed a significant activity (88.3-99.9% inhibition determined at 500 μM concentration). Structures of the synthesized compounds were confirmed by 1H-NMR, 13C-NMR, mass spectrometry and elemental analysis data.

Herein, we report the design and calculated molecular properties of ten existing azo Schiff bases 5a–h and 7a, b. On the basis of a hypothetical antibacterial pharmacophore, the structures are designed to interact with Gram-positive and Gram-negative bacteria. The in vitro biological evaluation of these compounds allowed us to point out new potential non-nucleoside hits, with MIC values in the range of 2–8 μg/ml active against Staphylococcus aureus and Bacillus subtilis. In contrast to Gram positive strains, no activity is noted in favor of Gram negative strains (Klebsiella pneumonia, Pseudomonas aeruginosa and Escherichia coli). The antibacterial activity of these azo Schiff bases is discussed on the basis of theoretical calculations by using Petra, Osiris and Molinspiration (POM) model. Petra, Osiris and Molinspiration (POM) together as a successful support in drug design: antibacterial activity and biopharmaceutical characterization of some azo schiff bases.

A new series of six chromone-derived compounds and their Cu(II) complexes have been synthesized and characterized by their physical, spectral and analytical data. The ligands and their Cu(II) complexes were screened for their in vitro antibacterial activity against four Gram-negative (Escherichia coli, Pseudomonas aeruginosa, Salmonella typhi, Shigella flexneri) and two Gram-positive (Bacillus subtilis, Staphylococcus aureus) bacterial strains by agar-well diffusion method. The ligands were found to exhibit either no or low-to-moderate activities against one or more bacterial species whereas, the Cu(II) complexes exhibited moderate-to-high activity. The ligands which were inactive before complexation became active upon complexation with the Cu(II) metal ion and less active became more active.

A new series of biologically active thienyl derived triazole Schiff bases and their oxovanadium(IV) complexes have been synthesized and characterized on the basis of physical (m.p., magnetic susceptibility and conductivity), spectral (IR, ¹H and ¹³C NMR, electronic and mass spectrometry) and microanalytical data. All the Schiff base ligands and their oxovanadium(IV) complexes have been subjected to in vitro antibacterial activity against four Gram-negative (Escherichia coli, Shigella flexneri, Pseudomonas aeruginosa, Salmonella enterica serover typhi) and two Gram-positive (Staphylococcus aureus and Bacillus subtilis) bacterial strains and, for in vitro antifungal activity against Trichophyton longifucus, Candida albican, Aspergillus flavus, Microscopum canis, Fusarium solani and Candida glabrata. Brine shrimp bioassay was also carried out to check the cytotoxic nature of these compounds.

Sulfonamide-derived new ligands, 4-({[(E)-(5-bromo-2-hydroxyphenyl)methylidene]-amino}methyl)benzenesulfonamide and 4-bromo-2-((E)-{4-[(3,4-dimethylisoxazol-5-yl)sulfamoyl]phenyl}iminiomethyl)phenolate and their transition metal [cobalt(II), copper(II), nickel(II) and zinc(II)] complexes were synthesized and characterized. The nature of bonding and structure of all the synthesized compounds were deduced from physical (magnetic susceptibility and conductivity measurements), spectral (IR, 1H and 13C NMR, electronic, mass spectrometry) and analytical (CHN analysis) data. The structure of the ligand, 4-bromo-2-((E)-{4-[(3,4-dimethylisoxazol-5-yl)sulfamoyl]phenyl} iminiomethyl)phenolate was also determined by X-ray diffraction method. An octahedral geometry was suggested for all the complexes. In order to evaluate the biological activity of the ligands and the effect of metals, the ligands and their metal complexes were screened for in vitro antibacterial, antifungal and cytotoxic activity. The results of these studies revealed that all compounds showed moderate to significant antibacterial activity against one or more bacterial strains and good antifungal activity against various fungal strains. Copyright © 2011 John Wiley & Sons, Ltd.

A new series of Schiff base ligands derived from sulfonamide and their metal(II) complexes [cobalt(II), copper(II), nickel(II) and zinc(II)] have been synthesized and characterized. The nature of bonding and structure of all the synthesized compounds has been explored by physical, analytical and spectral data of the ligands and their metal(II) complexes. The authors suggest that all the prepared complexes possess an octahedral geometry. The ligands and metal(II) complexes have been screened for their in vitro antibacterial activity against bacterial strains, Escherichia coli, Shigella flexneri, Pseudomonas aeruginosa, Salmonella typhi and for antifungal activity against fungal strains, Trichophyton longifusus, Candida albicans, Aspergillus flavus, Microsporum canis, Fusarium solani and Candida glabrata. These assays enabled the identification of the metal complexes as an effective antimicrobial agent with low cytotoxicity.

An n+–p–p+ structure was formed by depositing a thin Al layer on one side and a semitransparent Pd layer on other side of a p–Si wafer, and the diffusion length L was determined from the slope of short circuit current density Jsc vs. illumination intensity Pin characteristics by illuminating the p+ side with a laser light of wavelength λ = 789 nm, following the photocurrent generation method. The slope was found to decrease after the specimen was exposed to air for a few hours before the measurement. The present investigation revealed that the degradation of slope was owing to increase in surface recombination velocity S significantly, e.g. to 2800 cm/s for air exposure of 8 h, above its initial value 10 cm/s. This resulted from adsorption of moisture on Pd surface which decreases work function of Pd and lowers the accumulation potential barrier. The adsorbed water molecules could be removed from Pd surface by vacuum pumping and then S again became small and the slope regained its original value. The true value of L, smaller or larger than the wafer thickness, can be determined using single monochromatic illumination if S is known or has a negligibly small value, as in our case where the specimen was stored in vacuum. In our specimen we determined L = 56 μm when S was negligibly small. However, using the experimental slopes of Jsc–Pin curves at two monochromatic illuminations obtained by Sharma et al. we determined both S and L and found their values 1390 cm/s and 94 μm, respectively.

This research communication is toward the investigation of the antibacterial, antifungal and antioxidant activities of the synthesized compounds 1-(4′-O-β- d -glucopyranosyloxy-2′-hydroxyphenyl)-3-aryl-propane-1,3-diones (5a)–(5h). These compounds have been obtained by the interaction of α-acetobromoglucose with 1-(2′,4′-dihydroxyphenyl)-3-aryl-propane-1,3-diones (3a)–(3h) under anhydrous condition and at lower temperature. The structures of these newly synthesized O-β- d -glucopyranosides were established on the basis of chemical, elemental, and spectral analyses. Further, the compounds (5b), (5c), (5d) and (5g) showed potent antibacterial and antifungal activity. A good correlation was obtained between the theoretical predictions of bioavailability using Lipinski’s rule-of-five and experimental verification.

Cadmium Selenide (Cd 34 Se 66 ) thin films are deposited on a glass substrate using the thermal evaporation method at room temperature. The Cd 34 Se 66 films are characterized using XRD. The crystallite size of the film is calculated from XRD data, which is found as 29.61 nm as-deposited. It is also found that crystallite size of Cd 34 Se 66 changed after irradiation with N 2 and Nd:YAG laser. The changes in the optical properties of the films after irradiation with N 2 laser and Nd:YAG laser are also studied in the wavelength range of 300–700 nm and it is found that the optical band gap of the Cd 34 Se 66 films changed after laser irradiation.

5-Substituted-8-methyl-2H-pyrido[1,2-a]pyrimidine-2,4(3H)-dione and its anilines, amino pyridines and hydrazides derivatives were prepared in a good to excellent yields. In the first step 8-methyl-2H-pyrido[1,2-a]pyrimidine-2,4(3H)-dione (1) was prepared by reacting 4-methyl-2-aminopyridine, with diethylmalonate. Compounds substituted pyrido[1,2-a]pyrimidine-2,4(3H)-diones (PPMDO) (2)–(17) were prepared by condensing 8-methyl-2H-pyrido[1,2-a]pyrimidine-2,4(3H)-dione in the presence of triethylorthoformte (TEF) and dimethylformamide (DMF), with respective amino components viz. 2-aminoacetophenone, 3-aminoacetophenone, 4-aminoacetophenone, 2,4,6-trimethylaniline, 2-fluoroaniline, 3-fluoroaniline, 4-fluoroaniline, 2-aminothiophenol, 2-amino-4-methylpyridine, 2-amino-5-methylpyridine, 2-amino-5-nitropyridine, Benzoic hydrazide, 4-nitrobenzoic hydrazide, 4-bromobenzoic hydrazide, 4-chlorobenzoic hydrazide and 4-hydroxybenzoic hydrazide, respectively. The chemical structures of all the compounds were elucidated by IR, 1H-NMR, 13C-NMR and elemental analysis data. The synthesized compounds were screened for their in vitro urease inhibition activity, by the phenol hypochlorite method. These compounds were found to exhibit either no or low to moderate or significant activity. The compounds (9) and (14) showed comparatively much higher activity. However, the compound (9) was found to be the most active one. Of the synthesized compounds (2)–(17), two compounds (9) and (14) were found to be significantly more potent inhibitors of urease activity than the starting compound (1). The same two compounds also exhibited anti-urease activity comparable to thiourea, a standard urease inhibitor used in this study as a reference.