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Synthesis of the Zn, Mg, and LuOAc phthalocyanines (Pcs) containing sterically hindered 2,6-di-(tert-butyl)-4-methylphenol group were successfully achieved by the cyclotetramerization of the 4-[2,6-di-(tert-butyl)-4-methylphenoxy]phthalonitrile. All compounds were fully characterized by 1H and 13C NMR, infrared, elemental analysis, UV–Vis, and MALDI-TOF spectral data. The photo-physicochemical properties of the targeted molecules include fluorescence quantum yields, lifetimes, singlet oxygen generation, and photodegradation quantum yields were recorded in dimethyl sulfoxide.

A group of new substituted pyrimidine compounds, and their thiazolopyrimidines and 1,3,4-oxadiazolyl acyclic sugar derivatives have been synthesized as potential anti-cancer candidates. Oxadiazolyl-pyrimidine hybrid compounds have been synthesized by the reaction of thioacetohydrazide derivative with carbon disulfide and heterocyclization of sugar hydrazones with acetic anhydride. The synthesized products have been studied for their anticancer activity against human liver carcinoma (HepG-2) and human normal retina pigmented epithelium (RPE-1). The synthesized sugar hydrazine of D-glucose, its 1,3,4-oxadiazole acyclic nucleoside and arylidine derivative demonstrate high selective anti-cancer activity against liver cell line without side effects on normal cells.

A number of novel pyrrolo[3,2-c]carbazole-2-carbohydrazides5a–dwas prepared from readily available 6-methyl-1,6-dihydropyrrolo[3,2-c]carbazole-2-carboxylate3and underwent cyclodehydration to produce the corresponding 2-(6-ethyl-1,6-dihydropyrrolo[3,2-c]carbazol-2-yl)-1,3,4-oxadiazoles6a–dwithp-toluenesulfonyl chloride (p-TsCl) andN,N-diisopropylethylamine (DIPEA) as dehydrative reagents. The structures of the targeted compounds were confirmed through1H NMR,13C NMR, IR, mass spectrometry and single crystal X-ray diffraction techniques. Moreover, the antibacterial properties of the synthesized compounds were evaluated against colistin resistant (ColR)Klebsiella pneumoniae, ColRAcinetobacter baumannii,Pseudomonas aeruginosa,Escherichia coliandStaphylococcus aureus. Among the synthesized compounds,5dwas found to be active on ColRK. pneumoniae(MIC = 64 µg/mL) while compounds4(MIC= 6a(MIC==E. coli. Preliminary assay showed that the pyrrolo[3,2-c]carbazole-2-carbohydrazides and 2-(6-methyl-1,6-dihydropyrrolo[3,2-c]carbazol-2-yl)-1,3,4-oxadiazoles showed promising antibacterial activity on important nosocomial multi drug resistant (MDR) pathogens.

N'-(2-((4-(Benzo[d][1, 3]dioxol-5-yl)-3-cyano-6-(naphthalen-2-yl)-pyridin-2-yl)oxy)- acetyl)benzohydrazide (6) and hydrazide derivatives (7–10) were synthesized via reaction of 3-cyano-pyridinacetohydrazide (5) with benzoylchloride and the appropriate aldehyde, respectively. Also, 4-(Benzo[d][1, 3]dioxol-5-yl)-2-(2-(3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)-2-oxoethoxy)-6-(naphthalen-2-yl) nicotinonitrile (11) was prepared through reaction of (5) with ethylacetoacetate. In addition, the hydrazide 5 was used as a starting material for synthesizing other nicotinonitrile derivatives (12, 13) and acetohydrazides (14, 15). Moreover, new 2, 5-disubsitituted-1,3,4-oxadiazoles (16, 17) were furnished by the reaction of (5) with benzoic acid derivatives. The cytotoxicity for some new compounds was investigated against human breast cancer MCF-7 and MDA-MB-231 cell lines at concentrations (0, 10, 20, 40, 60, 80, and 100 μg/ml) using MTT assay. Compounds (4, 9, 14 and 17) were recorded the lowest half-maximal inhibitory concentrations (IC50s) against MCF-7 and MDA-MB-231 cell lines via cytotoxicity assays. These results were confirmed using molecular docking experiments. From the previous observations, we suggested that our synthesized compounds could be of great potential against breast cancer cells.

Most nanomedicines that attack tumors by Reactive Oxygen Species (ROS) based on lipid peroxidation mechanisms require external activation to work. The leading example is Photodynamic Therapy (PDT), for which an external light source stimulates ROS production. PDT has been utilized in the treatment of melanoma patients as part of palliative care, and it has shown promise in clinical trials. However, it has several limitations in terms of practical applications, such as inadequate photosensitizer (PS) dispersion, tumor-oxygenation dependency, and therapeutic escape in aggressive tumors. To overcome these obstacles, our targeted dual-modal PDT/Chemodynamic therapy (CDT) has produced promising results, with a stronger therapeutic impact than CDT or PDT alone. We herein report polymer nanoparticles functionalized with endothelin ligands (EDN3-CP nanocomposite) that are specifically designed to target melanoma tumors. The nanoparticles are intrinsically active against melanoma tumor cells even without the use of external light. The Iron in the EDN3-CP nanocomposite catalyzes the Fenton reaction in tumor cells, allowing for CDT. CDT produces ROS by converting endogenous hydrogen peroxide (H2O2), which is elevated in most tumor microenvironments (TME), to hydroxyl radicals (˙OH). The ˙OH that result can quickly oxidize bio-macromolecules, destroy DNA and kill tumor cells. The EDN3-CP nanocomposite is therefore not reliant on oxygen availability, making it a promising therapeutic option for hypoxic malignancies. Herein, the melanoma-targeted EDN3-CP nanocomposite demonstrated substantial PDT and CDT together with respect to Malme-3M and A375 melanoma cells. Our findings suggest that tumor cells that overexpress EDNRB, particularly melanoma cells, can be effectively targeted. Our data indicate that the EDN3-CP nanocomposite allows for ferroptosis-assisted CDT, paving the way to combine with PDT for maximized therapeutic efficacy as a new therapeutic approach to tumor treatment.

Different metal catalysts have been tested for the one-pot transformation of carbonyl compounds, amines and phosphites to α-aminophosphonates. The influence of catalyst type, amount, solvent and the substrate electronic factor have been investigated. The results revealed that the carbonyl compounds could be smoothly converted into α-aminophosphonates at room temperature in good to excellent yields, with or without solvent in a reasonable reaction time. These results suggested that among others, lithium perchlorate and metal triflates were proven to be effective catalysts in 10 moles % catalysts. Polar aprotic solvents proved to be the best for the synthesis of α-aminophosphonates. The synthesized compounds' structure characterizations were elucidated by different spectroscopic tools and showed results consistent with the expected structures.

A new range of sandwich type tetra and octa bis-phthalocyanines (Car-Pc2-1 and Car-Pc2-2) starting from commercially available N-ethylcarbazole were successfully prepared whereby two phthalocyanine moieties are connected with a lutetium ion. Structural characterization of Lu(III) bis phthalocyanines (Lu(III)bisPc) was performed by 1H NMR, 13C NMR, infrared (IR), UV-vis-NIR, and MALDI-TOF spectroscopic techniques. The electrochemical properties of bis-phthalocyanines were characterized using cyclic voltammetry (CV) and square wave voltammetry (SWV). Lu(III)bisPcs were then electropolymerized on glassy carbon electrodes (GCE). Furthermore, new modified electrodes with the electropolymerization of Lu(III) bisPc by doping with graphane were developed in order to detect low concentrations of ascorbic acid (AA), dopamine (DA) and uric acid (UA). The surface morphologies of the hybrid electrodes were investigated using SEM/EDX, UV-Vis, IR and Raman spectroscopies. The sensing behavior of the modified electrodes was also tested to detect AA, DA and UA analytes. The Grp/Car-Pc2-1/GCE electrode selectively detected AA with a limit of detection (LOD) of 1.56 μM, while LOD values of Ply(Car-Pc2-2)/GCE and Grp/Ply(Car-Pc2-2)/GCE were determined to be 0.16 μM and 1.07 μM for DA and UA, respectively, by voltammetric analyses. Moreover, the modified electrodes were also applied to detect AA, DA and UA in tap water samples using the standard addition method with satisfactory results.

Tetra substituted peripheral and non-peripheral Zn(II) phthalocyanines were successfully synthesized employing 4-(bis(3-methyl-1H-indol-2-yl)methyl)phenol as a starting material. The structure of these synthesized compounds was confirmed using 1H NMR, [Formula: see text]C NMR, infrared (IR), UV-vis, and MALDI-TOF spectral data. The photophysical (fluorescence quantum yields and lifetimes) and photochemical (singlet oxygen generation) properties of all synthesized peripheral and non-peripheral compounds were investigated in order to determine the potential of these compounds for application in photodynamic therapy.

New compounds based on Furanone derivatives were synthesized by reaction of 3-(4-nitrobezylidine)-5-phenylfuran-2(3H)-one with various reagents as malononitrile then D-glucose, thiosemicarbazide then D-glucose, ethyl acetoacetate, acetyl acetone, ethyl cyanoacetate, hydrazine hydrate/acetic acid, thiourea, o-phenylene diamine, hydrazine hydrate/ethanol then 2-naphthalene thionylchloride and/or thiourea. Also, 3-(4-nitrobezylidine)-5-phenylfuran-2(3H)-one was reacted with benzyl amine to afford the 1,3-dihydro-2H-pyrrol-2-one derivative which was reacted with hydroxyl amine and/or phenyl hydrazine to afford compounds the oxazole and/or pyrazole derivatives respectively. Finely, 6-(4-nitrophenyl)-5-(2-oxo-2-phenylethyl)-2-thioxotetrahydro-pyrimidin-4(1H)-one was allowed to react with 2-oxo-N-phenylpropanehydrazonoyl chloride yielding [1,2,4]triazolo[4,3-a]pyrimidin-7(1H)-one derivative. The anti-cancer activity of some of some of the new synthesized compounds towards breast carcinoma cells (MCF-7) was evaluated that demonstrated good to moderate results. Also, we had evaluated the cytotoxicity of the new tested compounds against the normal cells (MRC-5) which showed low toxicity on them.

Background Parkinson's disease (PD) is a common neurodegenerative disorder characterized by progressive loss of nigrostriatal dopaminergic neurons leading to dopamine depletion and problems of movement, emotions, and cognition. While the pathogenesis of PD is not clear, damage of dopaminergic neurons by oxygen-derived free radicals is considered an important contributing mechanism. This study aimed to evaluate the role of treadmill exercise in male Wister rats as a single treatment and as an aid-therapy with L-dopa for rotenone-induced PD. To study the role of the Nrf2- ARE pathway as a mechanism involved in exercise-associated improvement in rotenone-induced PD in rats. Method Animals were divided into 5 groups, (Control, rotenone, rotenone\exercise, rotenone\L-dopa, and rotenone\exercise\L-dopa (combination)groups). After the PD induction, rats in the rotenone\exercise and combination groups were daily treadmill exercised for 4 weeks. Results Treadmill exercise significantly improved behavioral and motor aspects of rotenone-induced PD. When treadmill exercise was introduced as a single intervention, it amended most behavioral aspects of PD, gait fully corrected, short-term memory, and motor coordination. Where L-dopa corrected locomotor activity and motor coordination but failed to improve short-term memory and only partially corrected the gait of rotenone-treated rats. When treadmill exercise was combined with L-dopa, all features of PD were corrected. It was found that exercise upregulated some of its associative genes to Nrf2 pathways such as TFAM, Nrf2 and NQO.1 mRNA expression. Conclusion This study suggests that forced exercise improved parkinsonian like features by activating the Nrf2 pathway.

3-(2-Thienyl)-5-aryl-1-thiocarbamoyl-2-pyrazolines were reacted with chloroacetone derivatives and hydrazonyl chloride derivatives in ethanol to afford the corresponding thiazolylpyrazoline derivatives and thiophenylpyrazolyl-5-substituted aryl-diazenylthiazole derivatives, respectively. The structures of the newly synthesized compounds were elucidated by different elemental and spectral analyses (IR, mass, 1H and 13C NMR). The antimicrobial and antifungal activities of the newly synthesized compounds were evaluated against four bacterial species and five fungal strains. In addition, the antitumor activities of two of the newly synthesized compounds 1-(2-(5-(4-chlorophenyl)-3-(thiophen-2-yl)-4,5-dihydropyrazol-1-yl)-4-methyl thiazol-5-yl)ethan-1-one and 2-(5-(4-chlorophenyl)-3-(thiophen-2-yl)-4,5-dihydro-1H-pyrazol-1-yl)-4-methyl-5-(phenyl-diazenyl)thiazole against HEPG-2, HCT-116, MCF-7, BHK, and CACO-2 were evaluated. From the obtained results, we found that these two compounds were the most potent candidates towards all gram-positive and gram-negative bacteria, as well as the fungi studied. Also, the same two compounds showed strong antitumor activities against two of the tumor cell lines (HCT-116 and CACO-2).

Potential influences of soil inoculation using phosphate-solubilizing bacteria (PSB) in integration with or without foliar spraying using mono-ammonium phosphate (MAP) or nano-phosphorus (NP) on performances, physio-biochemical attributes, and antioxidative defense system components in Phaseolus vulgaris plants were identified. A greenhouse preliminary and main pot experiments were conducted in calcareous soil (22% CaCO3) during fall and summer seasons of 2017/2018 and 2018/2019 in a completely randomized design. Preliminary experiments showed that the four concentrations: 1.0, 0.1, 0.5, and 0.05 g L−1 were the best for MAP, NP, and MAP when applied in integration with PSB, and NP when applied in integration with PSB, respectively, yielding the best results for plant growth and yield, total chlorophylls and P contents, and PSII efficiency (Fv/Fm). Therefore, these concentrations were selected for the main study. In main experiments, soil PSB or foliar MAP or NP resulted in significant increases in plant growth and yields, photosynthetic efficiency, gas exchange, relative water content, membrane stability index, ascorbate (AsA) and glutathione (GSH) contents and their redox states, contents of P, soluble sugars, glycine betaine, and activities of proline dehydrogenase (ProDH), superoxide dismutase (SOD), catalase (CAT), glutathione S-transferase (GST), ascorbate peroxidase (APX), glutathione reductase (GR), monodehydroascorbate reductase (MDHAR), and dehydroascorbate reductase (DHAR) compared to controls. In contrast, oxidative stress biomarkers (electrolyte leakage, lipid peroxidation, superoxide, and hydrogen peroxide), contents of proline and P5C, and activities of P5SC and phosphatase were significantly reduced. However, integrative PSB+MAP or PSB+NP treatment further improved all abovementioned parameters in plants. Integrative PSB+NP was the best treatment, awarding best improvements in all investigated parameters. Therefore, it can be recommended for cultivation and sustainability of Phaseolus vulgaris crop in calcareous soils.

Novel peripherally and non-peripherally 3-methylindole-substituted zinc phthalocyanine derivatives were synthesized as photosensitizers for photodynamic therapy in cancer treatment. The photophysical, photochemical and photobiological properties of targeted phthalocyanines were also investigated. For this purpose, the fluorescence and singlet oxygen quantum yields, and fluorescence lifetime values of the final compounds were determined in DMF solutions. The phototoxicity and cytotoxicity of the phthalocyanine complexes were tested against the invasive human breast cancer cell line (MDA-MB-231) for determination of their photosensitizing ability in the area of photodynamic therapy. It was revealed that while peripherally 3-methylindole-substituted phthalocyanine was found to be toxic for cells in both dark and light conditions, its non-peripherally substituted phthalocyanine analogue significantly caused cell death following light irradiation. A preliminary assay suggested that the non-peripherally linked phthalocyanine could be a suitable candidate for cancer treatment via photodynamic therapy techniques.

In the past decade, the use of marine mussels as seafood is being more popular. They considered being a rich source of various nutritional bioactive compounds that aroused the scientific community's interest. This study investigated the antioxidant and the antithrombotic consequences on Sprague-Dawley male rats after adding dried New Zealand mussel Perna canaliculus in their diet. The biochemical, hematological and histopathological changes were also observed. Forty rats were divided into four groups according to the amount of dried mussels in their diet, in addition to a control group that consumed a basal diet only. Group 1 consumed 25% dried mussels in its basal diet; Group 2 consumed 35% dried mussels in its basal diet, and Group 3 was consumed 45% dried mussels in its basal diet. The biochemical parameters showed improvements in liver function. Interestingly, the lipid profile decreased, especially the low-density lipoprotein cholesterol (LDL-C) levels which were reduced significantly in Group 3 (p < .01). These observations were accompanied by a decrease in iron levels significantly as the amount of dried mussels increased (p < .01). Furthermore, the noticed changes in the hematological profile prove that there is an increase in antithrombotic activity. Dried mussels had potent antioxidant effects in the liver as shown by increased lipid peroxide (p < .05), reduced glutathione (p < .05), and glutathione peroxidase (GSH-Px; p < .05). Additionally, antioxidant activity in the kidney was shown to increase through GSH-Px activity (p < .01). In conclusion, these results indicate that consuming dried mussels resulted in improved biochemical and antioxidants activities and could be used as an antithrombotic agent.

New pyridine, pyrazoloyridine, and furopyridine derivatives substituted with naphthyl and thienyl moieties were designed and synthesized starting from 6-(naphthalen-2-yl)-2-oxo-4-(thiophen-2-yl)-1,2-dihydropyridine-3-carbonitrile (1). The chloro, methoxy, cholroacetoxy, imidazolyl, azide, and arylamino derivatives were prepared to obtain the pyridine-−C2 functionalized derivatives. The derived pyrazolpyridine-N-glycosides were synthesized via heterocyclization of the C2-thioxopyridine derivative followed by glycosylation using glucose and galactose. The furopyridine derivative 14 and the tricyclic pyrido[3′,2′:4,5]furo[3,2-d]pyrimidine 15 were prepared via heterocyclization of the ester derivative followed by a reaction with formamide. The newly synthesized compounds were evaluated for their ability to in vitro inhibit the CDK2 enzyme. In addition, the cytotoxicity of the compounds was tested against four different human cancer cell lines (HCT-116, MCF-7, HepG2, and A549). The CDK2/cyclin A2 enzyme inhibitory results revealed that pyridone 1, 2-chloro-6-(naphthalen-2-yl)-4-(thiophen-2-yl)nicotinonitrile (4), 6-(naphthalen-2-yl)-4-(thiophen-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-amine (8), S-(3-cyano-6-(naphthaen-2-yl)-4-(thiophen-2-yl)pyridin-2-yl) 2-chloroethanethioate (11), and ethyl 3-amino-6-(naphthalen-2-yl)-4-(thiophen-2-yl)furo[2,3-b]pyridine-2-carboxylate (14) are among the most active inhibitors with IC50 values of 0.57, 0.24, 0.65, 0.50, and 0.93 µM, respectively, compared to roscovitine (IC50 0.394 μM). Most compounds showed significant inhibition on different human cancer cell lines (HCT-116, MCF-7, HepG2, and A549) with IC50 ranges of 31.3–49.0, 19.3–55.5, 22.7–44.8, and 36.8–70.7 μM, respectively compared to doxorubicin (IC50 40.0, 64.8, 24.7 and 58.1 µM, respectively). Furthermore, a molecular docking study suggests that most of the target compounds have a similar binding mode as a reference compound in the active site of the CDK2 enzyme. The structural requirements controlling the CDK2 inhibitory activity were determined through the generation of a statistically significant 2D-QSAR model.

Background & Objective:New diaryl-substituted pyrimidinedione compounds, their thioxo derivatives as well as their bicyclic thiazole compounds were synthesized and characterized.Methods:The glycosylamino derivatives of the synthesized disubstituted derivatives of the pyrimidine scaffold were also prepared via reaction of the N3-amino derivatives with a number of monosaccharides followed by acetylation.Results:The anticancer activity of the synthesized compounds was studied against human liver cancer (HepG2) and RPE-1cell lines. Compounds 2a, 2b, 3a and 12 showed potent activities with IC50 results comparable to that of doxorubicin.Conclusion:Docking investigations into Cyclin-dependent kinase 2 (CDK-2) enzyme, a potential target for cancer medication, were also reported showing the possible binding interaction into the enzyme active site to support their activity behavior.

New piperidinone incorporating pyrimidine, triazine, diazipine, oxatriazine, and thiazole derivatives have been synthesized starting with tetramethylpipridin-4-one. Structures of the newly synthesized compounds are characterized on the basis of spectroscopic and analytical data. The anticancer activity of the prepared compounds has been studied in vitro against HCT-116 and MCF-7 human cancer cells using the MTT assay. A number of compounds demonstrates potent activity towards both cell lines with IC50 values comparable with doxorubicin.

New sugar hydrazones incorporating furan and/or 1,3,4-thiadiazole ring systems were synthesized by reaction of the corresponding hydrazide with different aldose sugars. Heterocyclization of the formed hydrazones afforded the derived acyclic nucleoside analogues possessing the 1,3,4-oxadiazoline as modified nucleobase via acetylation followed by the heterocyclization process. The anticancer activity of the synthesized compounds was studied against human liver carcinoma cell (HepG-2) and at human normal retina pigmented epithelium cells (RPE-1). High activities were revealed by compounds 3, 12 and 14 with IC50 values near to that of the reference drug doxorubicin.

A range of novel 4,6-dimethoxy-1H-indole-2-carbohydrazides was prepared starting from methyl 4,6-dimethoxy-1H-indole-2-carboxylate which underwent cyclodehydration to generate the corresponding 2-(indol-2-yl)-1,3,4-oxadiazole scaffolds in the presence of N,N-diisopropylethylamine and p-toluenesulfonyl chloride in acetonitrile. All novel compounds were fully characterized by 1H NMR, 13C NMR, FT-IR, and high-resolution mass spectroscopic data. Biological importance of the designated compounds was identified by employing three different antioxidant property determination assays, namely DPPH free radical scavenging, ABTS cationic radical decolarization, and cupric reducing antioxidant capacity (CUPRAC). The anticholinesterase properties were also evaluated by the acetylcholinesterase and butyrylcholinesterase enzyme inhibition assays. According to the results, the indole compounds possessing carbohydrazide functionality were found to be more promising antioxidant targets than the 2-(indol-2-yl)-1,3,4-oxadiazole systems. Nʹ-Benzoyl-4,6-dimethoxy-1H-indole-2-carbohydrazide, a member of the dimethoxyindole-2-carbohydrazide group, demonstrated a better inhibition performance than the standards. Additionally, extremely important results were obtained in the anticholinesterase enzyme inhibition assays in the case of 2-(indol-2-yl)-1,3,4-oxadiazole derivatives.

Utilizing Schiff base condensation of the 9-ethylcarbazole-3,6-dicarbaldehyde and thiosemicarbazides, four new N-ethylcarbazole-based bis-thiosemicarbazone compounds 4a–d were successfully synthesized in high yields. The photophysical properties of the targeted compounds 4a–d were investigated using UV–vis absorption and fluorescence emission spectroscopy. The antioxidant properties of targeted compounds 4a–d were determined by DPPH radical scavenging, ABTS Cation Radical Decolarization and CUPRAC Cupric Reducing Antioxidant Capacity assay methods. Moreover, the anti-cholinesterase properties of designated compounds were investigated by the Acetylcholinesterase (Ach) and Butyrylcholinesterase (BCh) enzyme inhibition assays. The compound 4a was determined as a valuable candidate to be a potent antioxidant agent for the DPPH and ABTS assays. The compound 4d was found to be a target compound for the kinetic measurements to identify the mechanism of action in the area of anticholinesterase activity assay.

The synthesis and characterization of meso-piperidine linked Bodipy starting from 4-(2-(piperidine-1-yl)ethoxy)benzaldehyde was described. Meso-piperidine linked Bodipy was subsequently used for the construction of distyryl-piperidine-Bodipy and distyryl-morpholine-Bodipy via Knoevenagel type reaction. The photophysical properties including molar extinction coefficient, fluorescence lifetime and fluorescence quantum yield of Bodipys were investigated in ethanol solution. The targeted compounds were also assessed in live cell imaging and cytotoxicity studies by using breast cancer cell line, MCF-7 in vitro.

Acylation reactions of 4,6-dimethoxyindoles with glyoxyloyl chlorides were achieved by the use of graphite powder in 1,2-dichloroethane at reflux. The products were monoketones as a result of decarbonylation, rather than the expected 1,2-diketones. Treatment of these monoketones with base led to their cyclisation and elimination of methanol to afford the novel dipyrrolo[2.3-a:1′,2′,3′-fg]acridin-12(1H)-ones.

Efficient removal of Cd(II) and Pb(II) from contaminated water is considered a fundamental point of view. Synthetic hydrogel biopolymers based on chitosan and alginate (cost-effective and eco-friendly) were successfully designed and characterized by highly efficient removal contaminants. The sorbents are characterized by FTIR, SEM-EDX, TGA, XPS analyses and textural properties which are qualified by N2 adsorption. The sorption properties are firstly investigated by the effect of pH, sorption isotherms, uptake kinetics, and selectivity from multi-metal solution with equi-molar concentration. The sorbent with 1:3 ratios (of chitosan and alginate respectively) is the most effective for metal removal (i.e., 0.81 mmol Cd g−1 and 0.41 mmol Pb g−1). Langmuir and Sip’s models fitted better the adsorption isotherms compared to the Freundlich model. Uptake kinetics was well fitted by pseudo-first-order rate equation, while the saturation was achieved within 40 min. The sorbent shows good reproducibility through duplicate the experiments with negligible decreasing efficiency (&gt, 2.5%). The sorbent was applied for water treatment on samples collected from the industrial area (i.e., 653 and 203 times over the MCL for Cd(II) and Pb(II) respectively according to WHO). The concentration of Cd and Pb was drastically decreased in the effluents as pH increased with removal efficiency up to 99% for both elements at pH 5.8 and SD equivalent 1 g L−1 for 5 h.

The main idea in this research used quercetin (QT) as a stabilizing agent to prepare CuO nanoparticle (NPs). QT is a pigment which exists from plants, fruits, and in some medicines. It contains numerous hydroxyl groups, works as a complexing agent and a self-assembly agent. The prepared CuO-NPs were characterized by fourier transformed infrared (FT-IR), X-ray diffraction (XRD), scanning and transmission electron microscopy (SEM and TEM), and energy-dispersive X-ray analysis (EDX). The structure investigation confirm that the CuO-NPs were polycrystalline nature having a monoclinic crystalline form and showed (111) and (111) preferential orientations. The estimated particle sizes by XRD, TEM, and SEM ranged from 12.03 to 15.3 nm. Surface analysis displayed that homogeneously distributed CuO-NPs with a spherical shape. On the other hand, the synthesized CuO-NPs were tested for anticancer activity on the human Breast. The infected cell (MCF-7) uses MTT (3-(4,5-dimethyl-2-triazolyl)-2,5-diphenyl-2-tetrazolium bromide) test. The inferred CuO-NPs clarify high anticancer cytotoxicity of the (MCF-7) with an IC50 μM value of 57.6 and 42.8 µg/mL for 24 and 72 h respectively.

Introduction: Tea is one of the most common famous drink used daily in many countries in the world. Green tea contains polyphenolic compounds as catechins, that contains epigallocatechin gallate (EGCG). The lowering of plasma cholesterol levels and blood pressure as well as improvement of insulin sensitivity and endothelial function by green tea. Aim of the work: Study the effect of green tea on obesity, blood lipid level and its effect on fatty liver. Materials and Methods: All animal procedures were approved by the ethical committee of Faculty of Medicine, Tanta University. Thirty male Albino rats in the range of 230–280 g body weight was used in this study. All subjects were kept in an animal room of Physiology Department of Faculty of Medicine, Tanta University, in a controlled temperature and 12:12 h light/dark cycle with free access to food and water. The animals were divided into 3 groups of 10 animals each. Group-1: the sham group (sham operated, no obesity). Group-2: the vehicle group (obesity induced rats treated with normal saline). Group-3: the ghrelin group (obesity induced rats treated with EGCG). Results: Body weight, fat deposits, adiposity index and serum cholesterol increased significantly in a time-dependent manner in obese and control animals but were higher in the obese group (HFD > SD). High fat diet caused significant increases in the serum cholesterol level indicating high body lipid and obesity but when EGCG was administered after the beginning of high fat diet, these elevations were significantly depressed. Conclusion: In conclusion, since the administration of EGCG increase lipolysis and the accumulation of neutrophils in the damaged hepatic tissue, this agent appears to play a cytoprotective role in the liver insulted by fatty infiltration with obesity. It seems likely that Green tea (EGCG) is put in consideration as a potential therapeutic agent against obesity and hyperlipidemia.

Liver fibrosis is associated with increased mortality and morbidity. However, there is not effective treatment so far. Vinpocetine (Vinpo) is a synthetic derivative of vinca alkaloid vincamine. Limited previous reports have shown some beneficial effects of Vinpo in different organ fibrosis, but the ability of Vinpo to inhibit liver fibrosis induced by thioacetamide (TAA) has not been reported, that is why we investigate the potential ability of this vinca alkaloid derivative to attenuate liver fibrosis. Hepatic fibrosis was induced in male Sprague Dawley rats by TAA (200 mg/kg; ip; 3 times/week) for 6 weeks. Daily treatments with Vinpo (10–20 mg/kg/day; orally) ameliorated TAA-induced hepatic oxidative stress and histopathological damage as indicated by a decrease in liver injury markers, LDH, hepatic MDA, and NOx levels, as well as increase anti-oxidative parameters. Besides, the anti-fibrotic efficacy of Vinpo was confirmed by decreasing hydroxyproline, and α-SMA. Also, the anti-inflammatory effect of Vinpo was explored by decreasing IL-6 and TNF-α levels. Our novel findings were that Vinpo decreased VEGF/Ki-67 expression in the liver confirming its effect on angiogenesis and proliferation. These findings reveal the anti-fibrotic effect of Vinpo against TAA-induced liver fibrosis in rats, and suggest the modulation of oxidative stress, inflammation, angiogenesis and proliferation as mechanistic cassette underlines this effect.

Authigenic carbonates represent a significant microbial sink for methane, yet little is known about the microbiome responsible for the methane removal. We identify carbonate microbiomes distributed over 21 locations hosted by 7 different cold seeps in the Pacific and Atlantic Oceans by carrying out a gene-based survey using 16S rRNA- andmcrA gene sequencing coupled with metagenomic analyses. These sites were dominated by bacteria affiliated to the Firmicutes, Alpha- and Gammaproteobacteria. ANME-1 and −2 clades were abundant in the carbonates yet their typical syntrophic partners, sulfate reducing bacteria, were not significantly present. Our analysis indicated that methane oxidizers affiliated to the ANME-1 and −2 as well as to theCandidatusMethanoperedens clades, are capable of performing complete methane- and potentially short-chain alkane oxidations independently using oxidized sulfur and nitrogen compounds as terminal electron acceptors. Gammaproteobacteria are hypothetically capable of utilizing oxidized nitrogen compounds in potential syntrophy with methane oxidizing archaea. Carbonate structures represent a window for a more diverse utilization of electron acceptors for anaerobic methane oxidation along the Atlantic and Pacific Margin.

6-(4-Chloro-3-nitrophenyl)-4-oxo-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carbonitrile (4) was prepared and was reacted with ethyl chloroacetate, hydrazine hydrate, 4-chloroaniline, formaldehyde, acetic anhydride, formic acid, carbon disulfide, 4-cyanobenzaldehyde, triethyl orthoformate, D-sugars, 4-aminoacetophenone, benzoyl choride and cyclohexanone to afford a series of new uracil derivatives (5-18). Examination of some of the prepared compounds for their antimicrobial, antioxidant and anticancer activities was conducted. Among the tested samples, compound 17 was the most active substance against the gram-positive bacteria and was more potent than the reference drug Cefoperazone. Moreover, the antibacterial activity of 17 was higher against gram-negative bacteria. Compounds 6 and 13 reached a higher scavenging ability toward DPPH radicals and are better candidates for antioxidant activity. Also, compounds 6 and 13 had no significant anticancer activity toward liver cancer (Hep G2) and breast cancer (MCF-7) cell lines.

New N-substituted 5-(oxoindolinyl)-2-thioxothiazolidinone derivatives were synthesized. The C2- substituted thiazolidinone derivatives with piperidinyl and morpholinyl moieties in addition to the tetracyclic [(oxindolo) pyrazino] thiazolidine, the chloro-and amino-derivatives of the (indolyl) thiazolidinone ring system were also prepared. The COX-2 inhibition activity of the synthesized compounds was investigated by studying their ability to inhibit the conversion of arachidonic acid to prostaglandin H2 (PGH2). Five of the tested candidates, substituted (oxonidolyl) thiazolidine derivatives (3a, 6f, 8b, 10 and 12) showed significant COX-2 inhibitory activity exhibiting IC50 values better than or close to the reference celecoxib. The anti-inflammatory activity was studied revealing that a number of compounds have shown good activities and compound 10 produced no significant mucosal injury. Molecular docking study was implemented to interpret the variable inhibitory activity of the newly synthesized compounds against COX enzyme. The results suggested that some of these derivatives could be active COX inhibitors possessing a high preference for COX-2.

In this current work, 7-azaindole based 1,3,4-oxadiazoles have been successfully prepared by treatment of 3-(hydrazonomethyl)-7-azaindole with the different acyl chlorides or acetic anhydrides to give the corresponding carbohydrazides, followed by iodine mediated synthetic protocol in order to afford the corresponding 2,5-disubstituted 1,3,4-oxadiazoles. The full characterization data of the novel compounds were obtained by utilizing 1H NMR, 13C NMR, FT-IR, high-resolution mass spectrometry and single crystal X-ray diffraction techniques. The antioxidant activity and α-glucosidase inhibition potential of the prepared compounds are examined by in vitro assays. The targeted hydrazide linked 7-azaindoles and their corresponding cyclized form 1,3,4-oxadiazoles exhibited inhibitory potential with IC50 values ranges between 0.46 and 24.92 mM. Plausible binding mode and interaction of ligands with α-glucosidase enzyme have been studied by molecular docking, supporting the experimental results.

This work reports the synthesis and characterisation of reduced graphene-1,3,4-oxadiazole-2-thiol (rGS) as a novel nanocompound derivative for graphene. The preparation was performed through a series of reactions starting from graphene oxide, followed by incorporation of different proportions of this nanocompound with poly(vinyl alcohol) (PVA), via non-covalent bonding, to afford the rGS/PVA polymer composites. The pure rGS compound, rGS/PVA composite films and pure PVA film were characterised by different techniques including infrared (Fourier transform infrared) spectroscopy, scanning electron microscopy and powder x-ray diffraction. The electrical properties of the composite films, involving dielectric constant, permittivity ( ε′), imaginary permittivity ( ε″), conductivity (σAC) and loss factor tan δ, were investigated. The measurements were performed at frequencies of (5kHz to 0.5 MHz) at room temperature. At low frequency, the dielectric permittivity ( ε′) and imaginary permittivity ( ε″) attained higher values in all cases, although with increasing frequency these values diminished rapidly. It was also found that the alternating current conductivity of the composites increased with increasing frequency.

The unexpected result for the formylation of N-ethylcarbazole under the Vilsmeier–Haack conditions (POCl3/DMF) led to the synthesis of novel methylene bridged bis-pyrrolo[3,2-c]carbazoles via Hemetsberger indole synthesis was reported. A plausible mechanism for the formation of unexpectedly synthesized 7,7′-methylene bis(9-ethyl-9H-carbazole-3-carbaldehyde) 4 was postulated. The full characterization data of dicarbazolylmethane 4 and the bis-pyrrolo carbazoles 10a-b were obtained by utilizing 1H NMR, 13C NMR, FT-IR, mass spectrometry and single crystal X-ray diffraction techniques.

The current study was conducted on 70 male albino rats for elucidation the role of different green tea either local (E) or imported (C) and capsulated like green tea (CAP) as well as two common active principle Epigallocatechin gallate (EPI) and polyphenols (POL) on high fat ration (HFR) fed rats. The results showed that EPI and POL were showing a significant improvement in lipid profile and anti-oxidant status of rats. Meanwhile, EPI and CAP groups revealed the highest improvement in kidney function, while the Egyptian, Chinese green tea leaves and POL groups showed a significant enhancement in hepato-billiary system. All the studied groups revealed a significant improvement in cardiac function. Moreover, MEST relative expression increased in HFR group and showed a significant down-regulation in all green tea groups but EPI revealed the lowest relative expression in MEST which suggested its effect on improving obesity in rats.

Herein, a new analytical method for sensitive, rapid and reliable determination of two major trichothecenes: deoxynivalenol (DON) and T-2 toxin (T2) in maize and oats has been successfully established and validated. Acetonitrile/water mixture was used for sample extraction, and two solid phase extraction clean-up routes (i.e., Oasis HLB cartridges and MycoSep 227 columns) were investigated for optimal recoveries and adequate clean-up efficiency. The investigated mycotoxins were separated by ultra-performance liquid chromatography (UPLC) system and quantified by triple quadrupole mass spectrometry (MS/MS) using an electro spray-ionization interface (ESI) operating in positive polarity. MRM experiments were optimized for each trichothecene to generate high sensitive transitions. The method was validated according to European Union Directive: 2002/657/EC. Matrix-matched calibration demonstrated nice linearity in the concentration range of 5–200 µg/kg (T2) and 10–800 µg/kg (DON) with a coefficient of determination (R2) of >0.999. Fortified samples covering the same concentration ranges yielded average recovery values ranged from 85.0 to 95.3% with relative standard deviation (RSD) for the repeatability and reproducibility of

A new series of subphthalocyanine-borondipyrromethene scaffolds containing N -ethylcarbazole moiety have been successfully designed and synthesized. The identities of synthesized compounds were confirmed by using 1 H, 13 C NMR, matrix-assisted laser desorption/ionization time-of-flight mass spectrometry. The photophysical properties of the newly synthesized subphthalocyanine-borondipyrromethene conjugates were investigated via absorption and fluorescence spectroscopies in dichloromethane, tetrahydrofuran, benzene, and toluene solution (1 × 10 −5 M). The targeted compounds exhibit a highly efficient energy transfer process, either from the excited borondipyrromethene to the subphthalocyanine core or from the excited subphthalocyanine to the mono or distyryl borondipyrromethene unit. The time resolved fluorescence studies of the subphthalocyanine- borondipyrromethene conjugates were also examined.

Phage typically have small genomes and depend on their bacterial hosts for replication. DNA sequenced from many diverse ecosystems revealed hundreds of huge phage genomes, between 200 kbp and 716 kbp in length. Thirty-four genomes were manually curated to completion, including the largest phage genomes yet reported. Expanded genetic repertoires include diverse and new CRISPR-Cas systems, tRNAs, tRNA synthetases, tRNA modification enzymes, translation initiation and elongation factors, and ribosomal proteins. Phage CRISPR-Cas systems have the capacity to silence host transcription factors and translational genes, potentially as part of a larger interaction network that intercepts translation to redirect biosynthesis to phage-encoded functions. In addition, some phage may repurpose bacterial CRISPR-Cas systems to eliminate competing phage. We phylogenetically define major clades of huge phage from human and other animal microbiomes, oceans, lakes, sediments, soils and the built environment. We conclude that their large gene inventories reflect a conserved biological strategy, observed over a broad bacterial host range and across Earth’s ecosystems.

The synthesis of (6-ethyl-1,6-dihydropyrrolo[3,2-c]carbazol-2-yl)methanol 5 and (6-ethyl-6,11-dihydro-1H-dipyrrolo[3,2-c:2,3-g]carbazole-2,10-diyl)dimethanol 6 were achieved via the reduction of methyl pyrrolo carbazole carboxylate 3 and methyl dipyrrolo carbazole carboxylate 4, respectively. The structures of hydroxymethyl-pyrrolocarbazoles 5 and 6 were supported by FT-IR, matrix-assisted laser desorption/ionization time-of-flight mass spectrometry, H-1 and C-13 NMR spectroscopy. The photophysical properties of the targeted compounds 3-6 were investigated by employing absorption and fluorescence spectroscopy in different common organic solvents. Also, the fluorescence lifetime ((F)) of the compounds was measured utilizing a time-correlated single-photon counting technique in tetrahydrofuran. Antioxidant activities of compounds 3-6 were determined by employing three different assays, namely DPPH radical scavenging, ABTS cation radical decolarization and cupric reducing antioxidant capacity. The results revealed that the ABTS cationic scavenging activity assay was found to be the most sensitive method for the determination of inhibition values.

A series of novel 2-(pyridin-4-yl)quinazolin-4(3H)-ones bearing different heterocycle cores as potential PI3K inhibitors have been synthesized and evaluated via the MTT assay for their antiproliferative properties against selected HePG-2, MCF-7, and HCT116 cancer cell lines. Among them, compound 9 displayed significant activity against HePG-2 (IC50 = 60.29 ± 1.06 μM) comparable to doxorubicin as a reference anticancer drug (IC50 = 69.60 ± 1.50 μM). Kinase inhibitory assessment of target products against PI3K and docking studies revealed the promising binding affinities which match with the binding mode of the ligand, SW13 towards the active site of PI3K. Therefore, this work represents a promising matrix for developing novel potential anticancer candidates.

Objectives: In subjects with transmitted thymidine analogue mutations (TAMs), boosted PIs (PI/b) are often chosen to overcome possible resistance to the NRTI backbone. However, data to guide treatment selection are limited. Our aim was to obtain firmer guidance for clinical practice using real-world cohort data.Methods: We analysed 1710 subjects who started a PI/b in combination with tenofovir or abacavir plus emtricitabine or lamivudine, and compared their virological outcomes with those of 4889 patients who started an NNRTI (predominantly efavirenz), according to the presence of ≥1 TAM as the sole form of transmitted drug resistance.Results: Participants with ≥1 TAM comprised predominantly MSM (213 of 269, 79.2%), subjects of white ethnicity (206 of 269, 76.6%) and HIV-1 subtype B infections (234 of 269, 87.0%). Most (203 of 269, 75.5%) had singleton TAMs, commonly a revertant of T215Y or T215F (112 of 269, 41.6%). Over a median of 2.5 years of follow-up, 834 of 6599 (12.6%) subjects experienced viraemia (HIV-1 RNA >50 copies/mL). The adjusted HR for viraemia was 2.17 with PI/b versus NNRTI-based therapy (95% CI 1.88-2.51; P Conclusions: In this cohort, patients harbouring ≥1 TAM as the sole form of transmitted drug resistance gained no apparent virological advantage from starting first-line ART with a PI/b.

BackgroundMost glycomics studies have focused on understanding disease mechanisms and proposing serum markers for various diseases, yet the influence of ethnic variation on the identified glyco-biomarker remains poorly addressed. This study aimed to investigate the inter-ethnic serum N-glycan variation among US origin control, Japanese, Indian, and Ethiopian healthy volunteers.MethodsHuman serum from 54 healthy subjects of various ethnicity and 11 Japanese hepatocellular carcinoma (HCC) patients were included in the study. We employed a comprehensive glycoblotting-assisted MALDI-TOF/MS-based quantitative analysis of serum N-glycome and fluorescence HPLC-based quantification of sialic acid species. Data representing serum N-glycan or sialic acid levels were compared among the ethnic groups using SPSS software.ResultsTotal of 51 N-glycans released from whole serum glycoproteins could be reproducibly quantified within which 33 glycoforms were detected in all ethnicities. The remaining N-glycans were detected weakly but exclusively either in the Ethiopians (13 glycans) or in all the other ethnic groups (5 glycans). Highest abundance (p < 0.001) of high mannose, core-fucosylated, hyperbranched/hypersialylated N-glycans was demonstrated in Ethiopians. In contrast, only one glycan (m/z 2118) significantly differed among all ethnicities being highest in Indians and lowest in Ethiopians. Glycan abundance trend in Ethiopians was generally close to that of Japanese HCC patients. Glycotyping analysis further revealed ethnic-based disparities mainly in the branched and sialylated structures. Surprisingly, some of the glycoforms greatly elevated in the Ethiopian subjects have been identified as serum biomarkers of various cancers. Sialic acid level was significantly increased primarily in Ethiopians, compared to the other ethnicities.ConclusionThe study revealed ethnic-specific differences in healthy human serum N-glycome with highest abundance of most glycoforms in the Ethiopian ethnicity. The results strongly emphasized the need to consider ethnicity matching for accurate glyco-biomarker identification. Further large-scale study employing various ethnic compositions is needed to verify the current result.

A simple and efficient synthesis of novel zinc(II) phthalocyanines bearing triazole moieties was described. The synthetic approach for preparation of the phthalocyanines 1 and 13 was achieved by Schiff base condensation reaction of phthalocyanine tetracarbaldehydes 3 and 12 with 4-amino-4H-1,2,4-triazole 5 in tetrahydrofuran in reasonable yields. The photophysical and photochemical properties of the compounds 1, 3, 12 and 13 were recorded only in DMSO. The singlet oxygen generation ability of the targeted phthalocyanine Schiff bases were investigated in an attempt to understand their potential for photodynamic therapy (PDT) activity. Moreover, in vitro PDT application was performed against the MCF-7 and MDA-MB-231 invasive breast carcinoma cell lines. Preliminary assay showed that the compounds 1 and 13 possessed the phototoxicity and cytotoxicity, with a maximum of 30% MCF-7 cells dead following light irradiation. It was also revealed that the targeted phthalocyanines possess promising characteristic as photosensitizer towards tumor cells.

A novel on/off fluorescent indole/BODIPY-based Cu2+ chemosensor (3) was synthesized by Knoevenagel condensation of BODIPY derivative 1 with 2-methyl-indole-3-carbaldehyde 2. The identity of compound 3 was confirmed by 1H NMR, 13C NMR, FT-IR, matrix-assisted laser desorption/ionization time-of-flight mass spectrometry and single crystal X-ray diffraction techniques. Fluorescent chemosensor (3) is found to be highly selective and sensitive for detection of Cu2+ with a color change from purple to yellow. The optical sensor features for the Cu2+ complex of 3 were investigated by UV–Vis and fluorescence spectroscopy. The addition of Cu2+ caused quenching of fluorescence intensity and the detection limit was calculated to be 0.124 μM. Also, the stoichiometry ratio of 3+Cu2+ was obtained 2:1 by Job’s plot. Live cell image, flow cytometry and cytotoxic properties of compound 3 were examined.

Tetra and octa substituted novel zinc(II) phthalocyanines (3a and 5a) bearing carbazole groups were synthesized by cyclotetramerization of respective phthalonitrile derivatives (3 and 5). The zinc(II) phthalocyanines (3a and 5a) were converted into the water-soluble quaternized derivatives (3b and 5b) by utilizing dimethylsulphate as quaternizing agent. The synthesized novel compounds were confirmed thruogh FT-IR, UV-vis and MALDI-TOF mass spectroscopic data and elemental analysis as well. The photophysical (fluorescence quantum yields and lifetimes) and photochemical (singlet oxygen generation) properties of new phthalocyanines were determined in dimethylsulfoxide (DMSO). The photophysical and photochemical results were compared according to the number of the carbazole groups on the phthalocyanine core. Additionaly, in vitro photocytotoxicity of the targeted compounds were examined against to hepato cellular carcinoma (HuH-7) cancer cell line for determination of their photosensitizing ability.

Pyrrolocarbazole and dipyrrolocarbazoles have been synthesized via the Hemetsberger indole synthesis, starting from 9-ethyl carbazole-3-carbaldehyde and 9-ethylcarbazole-3,6-dicarbaldeyde, respectively. The pyrrolocarbazole structures were confirmed through 1 H NMR, 13 C NMR, IR, mass spectrometry and single crystal X-ray diffraction techniques. The targeted compounds showed potent in vitro cytotoxicity against human colon cancer HT29 cells.

أجريت هذه الدراسة بهدف بيان تأثير إضافة بعض مضادات الأكسدة الانزيمية (الكاتليز) والكلوتاثيون المختزل وخليطهما إلى مخفف Trisفي قابلية التجميد لثيران الهولشتاين بعد الحفظ بالتجميد لمدد مختلفة. استعمل في هذه الدراسة سبعة ثيران هولشتاين بأعمار تتراوح بين 2.5–3 سنة. جمع السائل المنوي بوساطة المهبل الاصطناعي بواقع قذفة واحدة/ثور/اسبوع. جُمع السائل المنوي الطازج للثيران جميعها (Pooled semen) وقُسمَ بالتساوي على المعاملات المختلفة وبإستعمال مخفف Tris. عدت المعاملة الأولى كمجموعة سيطرة في حين أضيف انزيم الكاتليز للمعاملة الثانية والكلوتاثيون المختزل للمعاملة الثالثة بتركيز 100 وحدة دولية/مل و0.2 ملي مول/مل إلى مخفف Tris وعلى التوالي، فضلاً عن توليفتهما وللتراكيز نفسها المذكورة للمركبين للمعاملة الرابعة. أجريت دراسة تاثير هذه الإضافات في قابلية تجميد السائل المنوي خلال مدد حفظ زمنية مختلفة، تجميد بعد 48 ساعة وشهر وشهرين وثلاثة اشهر. أظهرت النتائج أنّ إضافة انزيم الكاتليز إلى مخفف Tris في المعاملة الثانية أدت إلى زيادة معنوية عند مستوى (P

In this study, two different BODIPYs containing carbazole groups at the mesa position were designed and synthesized. All compounds were fully characterized by elemental analysis, FT-IR, matrix-assisted laser desorption/ionization time-of-flight mass spectrometry, H-1 and C-13 NMR spectroscopy. The photophysical properties of the new compounds were investigated by means of absorption and fluorescence spectroscopies in dilute dichloromethane solutions. We were also interested in the biological activity of these two novel carbazole-linked BODIPYs, particularly concerning their ability to inhibit human colon cancer HT29 cell lines. The photophysical studies revealed strong donor acceptor interaction between carbazole and BODIPY and follow the order compound 5 > compound 4. Also, preliminary assay showed that compound 5 possessed higher cytotoxic activity than compound 4, with IC50 values of 8.3 ng/mL and 21.7 ng/mL respectively. (C) 2015 Elsevier Ltd. All rights reserved.

A number of bis-indolyl imine helical structures has successfully been synthesized employing Schiff base reaction conditions starting from 4,6-dimethoxy-2,3-diphenylindole with different o-phenyl diamines as π-spacer bridged. The structures of targeted compounds were identified by FT-IR, mass, 1H and 13C NMR spectroscopy along with single crystal X-ray diffraction techniques. The ground state absorption properties of the bis-indolyl compounds were also investigated utilizing UV–Vis absorption spectroscopy. As the biological aspect of the synthesized compounds, the anticholinesterase potency was investigated towards the acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes. The highest inhibition was determined in the presence of compound 9 with the values of 89.21 and 96.06, better than standard Galantamine, for AChE and BChE, respectively.

The synthesized and sensing capability of two novel azaindole substituted mono and distyryl BODIPY dyes against bisulfate anion were reported. Structural characterizations of the targeted compounds were conducted by using matrix-assisted laser desorption/ionization time-of-flight mass spectrometry, 1H and 13C NMR spectroscopies. Photophysical properties of the azaindole substituted BODIPY compounds were investigated employing absorption and fluorescence spectroscopies in acetonitrile solution. It was found that the final compounds 3 and 4 exhibited exclusively selective and sensitive turn-off sensor behavior on HSO4- anion. Additionally, the stoichiometry ratio of the targeted compounds to bisulfate anion was measured 0.5 by Job's method. Also, density function theory was performed to the optical response of the sensor for targeted compounds. Furthermore, the cytotoxicity of Azaindole-BODIPYs was examined against living human leukemia K562 cell lines.