Search

A new series of pyrazole-quinoline hybrids were synthesized by a base-catalyzed cyclocondensation reaction through one-pot multi-component reaction, based on molecular hybridization techniques. All the compounds 10a-x were examined for in vitro antibacterial and anticancer activities. Enzyme inhibitory activities were carried out against FabH and EGFR. From the studied compounds, most of the compounds showed effective antibacterial as well as anticancer activity against used strains and cancer cell lines, respectively. The most potent inhibitory activity was displayed by compound 10r against EGFR and by compound 10i against FabH. Spatial arrangement of the molecule and their HOMO-LUMO was studied and explained by DFT theory, to evaluate plane angle respective to the core and substitutions. Docking studies indicated that compound 10r was bound to the active pocket of EGFR with hydrogen bond and π-H interaction with minimum binding energy and compound 10i was bound to the active site of FabH with hydrogen bond and π-H interaction having minimum binding energy. Based on their substitutions, the hypothetical plane arising in the molecule and their twist angles were related with their activities against EGFR and FabH as well as antibacterial and anticancer activities.

A new series of biquinoline-phenylthiazole hybrids were designed and synthesized by a base-catalyzed cyclocondensation through one-pot multicomponent reaction. All compounds were tested for in vitro antimicrobial and anticancer activities. Enzyme inhibitory activities of all compounds were carried out against FabH and EGFR. Majority of the synthesized compounds displayed promising antimicrobial as well as anticancer activity against used strains and cancer cell lines, respectively. All the compounds were tested for in vitro anticancer activities against two cancer cell lines A549 and Hep G2. Compound 9n (IC50 = 0.09 μM) against EGFR and (IC50 = 1.03 μM) against A549 kinase displayed the most potent inhibitory activity as compared to other member of the series. In the molecular modelling study, compound 9p was bound in to the active pocket of EGFR with two hydrogen bonds and one π-cation interactions having minimum binding energy ΔGb = -8.5626 kcal/mol. For FabH molecule 9u was found to be binding in the active pocket with minimum binding energy of -8.4033 kcal/mol.

A series of novel ‘drug-like’ small molecules based on 1H-benzo[d]imidazole derivatives bearing furan-2-yl, 4-piperidine and 5-aryl/aminoaryl substitutions were designed and synthesised. The key intermediate tert-butyl-4-(5-bromo-2-(furan-2-yl)-1H-benzo[d]imidazol-1-yl)piperidine-1-carboxylate (5) was synthesised via sequential reaction starting from 4-bromo-1-fluoro-2-nitrobenzene (1). The 5-aryl-substituted molecular library was generated via Suzuki–Miyura coupling of tert-butyl-4-(5-bromo-2-(furan-2-yl)-1H-benzo[d]imidazol-1-yl)piperidine-1-carboxylate (5) with various boronic acids while Buchwald coupling of 5 with various anilines generated the second molecular library of tert-butyl-4-(2-(furan-2-yl)-5-(arylamino)-1H-benzo[d]imidazol-1-yl)piperidine-1-carboxylates. The structures of all the newly synthesised compounds were confirmed by spectral analysis. The optimised procedure gives easy access to two new molecular libraries of 1H-benzo[d]imidazoles with operational simplicity and good yield.

In present work, the synthesis, characterization, antibacterial and anticancer activities of a novel series of 1H-pyrazolo[1,2-b]phthalazine-5,10-dione derivatives bearing 2-aryloxyquinoline nucleus (6a-l) is reported. In vitro antibacterial and anticancer activities against used strains and two cell lines A549 and HepG2 as well as enzyme inhibitory activities against EGFR and FabH were carried out. The most potent inhibitory activity against EGFR was displayed by compound 6l and against FabH by compound 6i. Docking studies showed that compound 6l was bound to the active pocket of EGFR with hydrogen bond and π-H interaction with minimum binding energy and compound 6i was bound to the active site of FabH with hydrogen bond and π-H interaction having minimum binding energy. DFT studies explained spatial arrangement as well as HOMO-LUMO to evaluate the plane angle. On the basis of their substitutions, these plane angles were then related with their activity against EGFR and FabH as well as antibacterial and anticancer activities.

An alkoxy benzamide derivatives are have been synthesized in four steps. Alkylation, halo phenol coupling, nitro group reduction and acid amine coupling gave in decent yield. Likewise, these targets were synthesized by coupling of 4-(3,4-dichlorophenoxy) aniline with N-(4-(3,4-dichlorophenoxy)phenyl)- 4-alkoxybenzamide by using (1-[bis(dimethylamino)methylene]-1H-1,2,3-triazolo[4,5-b]pyridinium 3-oxide hexa fluorophosphate, hexa fluorophosphate azabenzotriazole tetramethyl uronium) (HATU), N,N-diisopropylethylamine (DIPEA) in dimethylformamide (DMF) at 0 ºC to room temperature. Reduction of nitro group in the presence of 10% Pd/C, H2 (g) in MeOH at room temperature. Obtained in decent to excellent yield. Anti-tuberculosis activity of all synthesized derivatives (7a-l) was complete against the H37RV strain as per reported broth dilution method mentioned in experimental section. Bio-assay results showing that derivatives 7c, 7e and 7i exhibited exceptional activity against the H37RV strain with MIC value 62.5 μg/mL. Furthermore, other derivatives were showed poor potency against same strain when compared with standard drugs isoniazid and rifampicin.

Alteration in the pattern of epigenetic marking leads to cancer, neurological disorders, inflammatory problems etc. These changes are due to aberration in histone modification enzymes that function as readers, writers and erasers. Bromodomains (BDs) and BET proteins that recognize acetylation of chromatin regulate gene expression. To block the function of any of these BrDs and/or BET protein can be a controlling agent in disorders such as cancer. BrDs and BET proteins are now emerging as targets for new therapeutic development. Traditional drugs like enzyme inhibitors and protein–protein inhibitors have many limitations. Recently Proteolysis-Targeting Chimeras (PROTACs) have become an advanced tool in therapeutic intervention as they remove disease causing proteins. This review provides an overview of the development and mechanisms of PROTACs for BRD and BET protein regulation in cancer and advanced possibilities of genetic technologies in therapeutics.

Many researchers claim that graphene, a specially studied carbon allotrope, has a single layer of atoms organized in a two-dimensional honeycomb lattice. Because of its exceptional electronic and mechanical properties, it has a significant job to perform in redefining future technologies. Although graphene has made a major breakthrough to be considered for a wide area of applications, most of the interesting properties of graphene are still at the early stage of research. Graphene dependent attenuators and single and multi-frequency constructible antennas are designed employing the tunability of graphene. As the name indicates, the form of RF technology that uses electromagnetic fields for automatic identification purposes of tags attached to objects is termed as radio frequency identification (RFID). For years, the use of pricy raw materials and intricate fabrication processes in metal coating and metal based conductive inks in printed electronics kept the involved cost very high. So, it is inevitable to replace the existing fabrication process with cheaper materials and simpler techniques. Researchers assert that printed graphene has the potential to be a competent alternative for RFID applications.

Binary mixtures with both the components are non-mesogenic becomes an interesting and enlighten feature when they exhibit mesomorphism at ambient temperature. In the present study, we report five b...

Cancer is one of the most difficult diseases and causes of death for many decades. Many pieces of research are continuously going on to get a solution for cancer. Quinoline and isoquinoline derivatives have shown their possibilities to work as an antitumor agent in anticancer treatment. The members of this privileged scaffold quinoline and isoquinoline have shown their controlling impacts on cancer treatment through various modes. In particular, this review suggests the current scenario of quinoline and isoquinoline derivatives as antitumor agents and refine the path of these derivatives to find and develop new drugs against an evil known as cancer.

A simple one-pot synthesis of N-substituted benzimidazoles from aromatic carboxylic acids and aromatic 1,2-diamines in the presence of 1-[bis(dimethylamino)methylene]-1H-1,2,3-triazolo[4,5-b]pyridinium 3-oxide hexafluorophosphate/hydroxybenzotriazole (HATU/HOBT) and N,N-diisopropylethylamine in DMF at 100°C, featuring good to excellent yields and easy workup, is developed. The protocol can be scaled to gram quantities, and no chromatographic purification is required.

BackgroundMetals are one of the micro molecules required by living cell to do their biochemical functions. Out of a list of metals few are very important and useful to cells while few are required in very minute amount and their higher concentration harm or cause adverse effects on living forms. Copper and ferrous are commonly counted as essential metals to plant cells but sometimes their higher concentration is harmful to plant cells. Copper is commonly counted as important metal to plant cells but sometimes their higher concentration is harmful to plant cells.ResultsIt was found that higher concentration of copper and ferrous showed reduction in germination percentages and gemination time of investigated plant while chromium shown lethal impacts on seed germinationConclusionsIn the present study effects of copper, chromium and nickel was studied for total sugar and protein content of widely cultivated pulses i.e. Glycine max. Collectively present study showed that higher concentration of copper and nickel has adverse effects on Glycine max total sugar and protein content while chromium has lethal impacts at lower concentration also.

Effect of position isomer in newly synthesized two liquid crystalline series having nitro and chloro groups at terminal and lateral position, with imine and cinnamoyloxy linkages was studied. The nitro and chloro groups in the aromatic end of the molecule are interchanged with each other at terminal and lateral position, giving rise to positional isomers. All synthesized compounds were characterized with standard spectroscopic techniques, Infrared, Ultra-Violet and Proton magnetic resonance spectroscopy. The mesophase behaviour was observed by a Polarizing optical microscope equipped with a heating stage and was confirmed by Differential scanning calorimetry with respective transition enthalpies of mesophase transition. The mesogenic derivative of both prepared series showed nematic and smectic A mesophase. DFT method was used to obtain optimized geometry of the molecules. The optimized geometry was used to obtain the Molecular electrostatic potential map, dipole moment, HOMO-LUMO and twist angle of the prepared series. The interaction between the molecules was studied on the base of electrostatic potential and HOMO-LUMO. The phase transition of the present two series is compared with each other and with three structurally related compounds to evaluate the effect of planarity, central linkage and position of substitution on their mesophase behaviour.

Stimuli-responsive di-block copolymers viz. poly(N-isopropylacrylamide)m-block-poly(butyl-3-vinylimidazolium bromide)n [abbreviated as PNIPAMm-b-PBVIBn m = 50 and 100, n = 54 and 115] were synthesized using RAFT (Reversible addition−fragmentation chain-transfer) polymerization. Gel permeation chromatography (GPC) and nuclear magnetic resonance (1H NMR) spectroscopy were used to characterize the block copolymer. Turbidity data shows that the lower critical solution temperature (LCST) of PNIPAM is independent of the molecular weight. No LCST behavior was estimated for PBVIB58 in an aqueous media. The addition of 2.75 M NaCl brings LCST of PBVIB58 to room temperature. The cloud point temperature (CPT) of both the block copolymers increases with an increase in the degree of polymerization of PBVIB. Scattering techniques confirm the molecular state of all the homopolymers at 28 °C in the dissolved condition. With an increase in temperature and the presence of sodium chloride (NaCl), both the copolymers remain as aggregates with PNIPAM as a core and PBVIB as a shell. The reverse structure is formed via the addition of 10 mM sodium dodecyl sulfate (SDS) into PNIPAM100-b-PBVIB54 solution.

All the heritable alterations in gene expression and chromatin structure due to chemical modifications that do not involve changes in the primary gene nucleotide sequence are referred to as epigenetics. DNA methylation, histone modifications, and non-coding RNAs are distinct types of epigenetic inheritance. Epigenetic patterns have been linked to the developmental stages, environmental exposure, and diet. Therapeutic strategies are now being developed to target human diseases such as cancer with mutations in epigenetic regulatory genes using specific inhibitors. Within the past two decades, seven epigenetic drugs have received regulatory approval and many others show their candidature in clinical trials. The current article represents a review of epigenetic heritance, diseases connected with epigenetic alterations and regulatory approved epigenetic drugs as future medicines.

A two new homologous series of λ-shape to T-shape mesogenic azo diesters were synthesized, and their thermotropic properties were studied by differential scanning calorimetry and a hot-stage polarizing optical microscope. The difference between these two series is in the structure of terminal substituents methyl (–CH3) for series I and methoxy (–OCH3) for series II at one terminus. Structure variation from λ-shape to T-shape as we go from lower members to higher members is discussed. In the series I, methoxy to n-pentyloxy derivatives are non-mesogenic. n-hexyloxy derivative exhibits only monotropic nematic mesophase. n-heptyloxy to n-dodecyloxy derivatives exhibit monotropic smectic C mesophase. n-tetradecyloxy derivative exhibits enantiotropic SmA mesophase, whereas n-hexadecyloxy derivatives exhibit monotropic Smectic A mesophase. In series II, methoxy to n-hexyloxy derivatives are non-mesogenic. n-heptyloxy and n-octyloxy derivatives exhibit monotropic smectic C mesophase. Smectic A mesophase commences from the n-decyloxy derivative as a monotropic and persists up to the last member synthesized. The mesomorphic properties of the present series were compared with each other and with the structurally related mesogenic homologous series to evaluate the effect of methyl (–CH3)/methoxy (–OCH3) substituents as well as variation in the shape of the molecule by varying the alkoxy chain length of the bulky lateral substituent on mesomorphism.

The bovine serum albumin nanoparticles (BSA-NPs) were prepared using desolvation process, in an aqueous medium with acetone as a desolvating agent. The BSA nanoparticles were found within 50 to 75 nm range confirmed by dynamic light scattering and scanning electron microscope. The interaction of prepared BSA-NPs with Cu2+ yielded Cu2+ conjugated BSA-NPs (Cu-BSA-NPs) analyzed by the same techniques. Both have been studied for their comparative thermal and dye adsorption analysis where the later was found 40% greater for Cu-BSA-NPs than BSA-NPs. Molecular modelling showed the methylene blue and methyl orange interactions into the active pocket of BSA with H-acceptor with ΔGb = −1.8 and −3.0 kcal/mol respectively. Similarly the Cu-BSA-NPs have shown better DNA binding and antioxidant activities as compared to BSA-NPs estimated through absorption spectra and free radical mechanism. Presence of metal ion has facilitated the BSA NPs for trapping the free radicals in its hydrophobic as well as hydrophilic domains. Both have also been tested in vitro against MCF (Breast cancer) cell line for their anticancer nature where Cu-BSA-NPs have been found more effective. Antimicrobial in vitro minimal inhibitory concentration (MIC) evaluation has been assessed on the basis of zone of inhibition with gram +ve and gram -ve bacteria B. cereus (MTCC430), S. aureus (MTCC 737), and E.coli (MTCC443), K. pneumonia (MTCC3384) respectively. The association of Cu2+ has impacted more in growth inhibition of bacteria.

The biomorphic carbide (Bio-C) with highly interconnected pore-joined carbon structure consisting of three dimensional alignments was prepared based on balsa wood, a non-hazardous herbal stuff, resulting an economic, environment-friendly fabrication process. The balsa wood gives hierarchical natural porous structure after the hydrothermal process, which offers ample enlargement area for MnO2 and eliminates the aggregation of MnO2 particles. Evolution of structure, morphology, and porous properties from pristine carbonized wood to porous Bio-C/MnO2 was systematically studied. The electrochemical performance of the Bio-C/MnO2 composite has been studied in a flexible symmetric supercapacitor (FSC) using PVA/H2SO4 hydrogel as an electrolyte. The as-prepared Bio-C/MnO2 composite demonstrated staggering electrochemical output, which is majorly resulted due to the large amount of pore volume along with 3D hierarchical pores. Electrochemical study showed that the Bio-C/MnO2 composites used in FSC had a specific capacitance (sp. cap.) of 148 F.g−1 at current density of 0.8 A.g−1, and exhibited stable long cycle life with a capacitance retention ratio of 78.77 % after 10000 cycles. The Bio-C/MnO2 hybrid materials having three dimensional porous structures are excellent materials in the wide area of bendable power storage system.

The nicotine (NT) is an addictive substance and most common continuous consumption is from smoking cigarettes and dip chewing tobacco. The removal of excess NT is possible through molecular interaction mechanisms by using active molecular functional moieties. In this context, the physicochemical properties (PCPs) such as density (ρ, ±10−3 kg m−3), viscosity (η, ±10−4 mPa·s), surface tension (γ, ±0.01 mN m−1), friccohesity (σ, ±10−5 s·m−1), activation energy (Δμ2*, ±10−2 kJ mol−1) and molecular radii (r, ±0.01 nm), and acoustic study of intermolecular interactions of NT with glutamic acid (GA), ascorbic acid (AA), citric acid (CA), dextrose (DX), and honey (HN) prevailing in aqueous solution have been reported at 303.15 K. These PCPs revealed that the intermolecular hydrogen bonding (IHB) occurs between nitrogen (N) atom in pyridine moieties and GA, AA, CA, DX, and HN molecules in presence of water (W) for the reorientations of the two NT rings. The increasing concentration of NT with aqueous GA, AA, CA, DX, and HN, the PCPs also increases. Hence, PCPs data demonstrate that maximum HB interactions (HBI) between pyridine moieties and these all molecules increases with increasing concentration of NT in aqueous medium. These physicochemical characterizations of the structural dynamics with NT are attributed to the different structures of GA, AA, CA, DX and HN molecules around the pyridine ring moieties of NT.

New Schiff’s base derivatives 5a–j have been synthesized by reaction between 5-aryloxypyrazole-4-carbaldehydes 3a–j and 2-(2-methyl-5-nitro-1H-imidazol-1-yl)acetohydrazide 4 in the presence of nickel (II) nitrate as a catalyst in ethanol at room temperature with good yield (75–88 %). All compounds were tested for antibacterial properties and inhibition of E. coli FabH. Of the compounds studied, the majority of the compounds showed effective antibacterial properties and inhibition of E. coli FabH activity. Compound 5i showed the most effective inhibition (IC50 = 4.6 ± 0.2 µM) by binding into the active site of the E. coli FabH receptor with minimum binding energy (ΔG b = −54.2961 kcal/mol). The binding was stabilized by two hydrogen bonds, two π–π, and three π–cation interactions.

Many reports implied that the BRAF serine/threonine kinase was mutated in various types of human tumors, which were related with cell growth, survival and differentiation. To provide new therapeutic opportunities, a series of novel 4,5-dihydro-1H-pyrazole derivatives (6a-10d) containing thiazole moiety as potential V600E mutant BRAF kinase (BRAF(V600E)) inhibitors were designed and synthesized. All compounds were evaluated in vitro for anticancer activities against WM266.4 human melanoma cell line and breast cancer MCF-7 cell line. Compound 10d displayed the most potential antiproliferative activity with an IC50 value of 0.12μM against cell line WM266.4 and 0.16μM against MCF-7 with positive control Sorafenib. Results of the inhibitory activity against BRAF(V600E) revealed that compound 10d was bearing the best bioactivity with IC50 of 0.05μM as well. On the basis of the result of flow cytometry, with the dose of compound 10d increasing, more and more cancer cell gradually encountered apoptosis or died, which indicated the compound 10d could induce remarkable apoptosis of MCF-7 and WM266.4 cells in a dose dependent manner. Furthermore, docking simulation of inhibitor analogues and 3D-QSAR modeling provided potential binding model and further knowledge of pharmacophore.

A new series of pyrazole–quinoline–pyridine hybrids were designed based on molecular hybridization technique and synthesized by a base-catalyzed cyclocondensation reaction through one-pot multicomponent reaction. All compounds were tested for in vitro antibacterial and anticancer activities. Enzyme inhibitory activities of all compounds were carried out against FabH and EGFR. Of the compounds studied, majority of the compounds showed effective antibacterial as well as anticancer activity against used strains and cancer cell lines respectively. Compound 7k (IC50 = 0.51 ± 0.05 μM) against EGFR and 7b displayed the most potent inhibitory activity with IC50 of 3.1 μM against FabH as compared to other member of the series. In the molecular modeling study, compound 7k was bound in to the active pocket of EGFR with three hydrogen bond and one π–cation interaction with minimum binding energy ΔGb = −54.6913 kcal/mol, as well as compound 7b was bound in to the active site of FabH with hydrogen bond and π–sigma interactions with minimum binding energy ΔGb = −45.9125 kcal/mol.

Herein we report the thermal, morphological, topographical, gas adsorption and biological activities of newly synthesized [Fe(CN)6]4−/[Fe(CN)6]3− based MOIFs using Differential Scanning Colorimetry (DSC), Scanning Electron Microscope (SEM), BET (Brunauer, Emmett and Teller) and spectrophotometric methods. Thermal analysis revealed an effect of MOIFs alkyl chain on their heat holding capacity as a function of temperature. Nitrogen adsorption method was applied for surface and apparent cross-sectional area determination within MOIF ionic assembly. The DNA binding activity (DBA) of as prepared MOIFs was found in 40% order, computed using Ameta-Hyper-Hypochromic model. The increments and decrements in DNA helix axial length were conferred by hydrophobic (Hb)/hydrophilic (Hp) interactions, attributing for corresponding hyper/hypo chromic effect. Considerable anticancer activities of +2 and +3 Fe oxidation states (evaluated on MCF-7 cell line) for the DTAB stabilized MOIFs, were noticed. Apart from this, the free radical antioxidant activity of MOIF has also been investigated, found as directly varying with the alkyl chain lengths. A free radical trapping mechanism is suggested on the basis of Hb-Hb and Hp-Hp interactions.

Series of novel Schiff's base derivatives have been synthesized by combining 2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethyl 4-formylbenzoate 5, 6 with aromatic/heterocyclic amine 7a–r, 8, 9a–r in ethanol. All compounds were evaluated for antibacterial assay and inhibition against E. coli FabH. Among the compounds studied, most of the compounds showed effective antibacterial and potential inhibitory activity against E. coli FabH. Compound 10q showed most potent inhibitory activity (IC50 = 2.6883 μM) by binding tightly to the active site of the E. coli FabH receptor with minimum binding energy (ΔGb = −55.3117 kcal mol−1), in which molecular docking study indicated the binding mode was stabilized by one hydrogen bond and five π–π interactions.

A series of new Schiff’s base derivatives 4a–x bearing 2-thiophenoxyquinoline nucleus have been designed and synthesized by reaction of 2-thiophenoxyquinoline-3-carbaldehydes 2a–d with various benzohydrazides 3a–f in the presence of Ni(NO3)2·6H2O as a catalyst. In vitro antibacterial screening was carried out against two Gram-positive bacteria (Bacillus subtilis ATCC 6633 and Staphylococcus aureus ATCC 6538) and two Gram-negative bacteria (Escherichia coli ATCC 35218 and Pseudomonas aeruginosa ATCC 13525). Of the compounds studied, compound 4e showed chief activity (MIC = 3.13 μg/mL) against S. aureus, and compounds 4p, 4k, and 4w were found to possess effective antibacterial activity against employed strains compared with standards used. The structures of Schiff’s base derivatives were established by using various spectroscopic methods. A crystal structure of compound 4k has been determined by X-ray diffraction analysis.

A new series of 4H-chromene derivatives 6a–x bearing 2-aryloxyquinoline nucleus have been synthesized under microwave irradiation by reaction of 2-aryloxyquinoline-3-carbaldehyde 3a–l, malononitrile 4, and compounds (Cyclohexanedione, Dimidone) 5a–b in the presence of NaOH as the basic catalyst. All the compounds were screened against three Gram-positive bacteria (Streptococcus pneumoniae, Clostridium tetani, Bacillus subtilis), three Gram-negative bacteria (Salmonella typhi, Vibrio cholerae, Escherichia coli) and two fungi (Aspergillus fumigatus, Candida albicans) using the broth microdilution MIC (Minimum Inhibitory Concentration) method. Upon study of the antimicrobial screening, it has been observed that a majority of the compounds were found to be active against C. tetani and B. subtilis as well as against C. albicans as compared to the standard drugs.

A new series of pyrano[4,3-b]pyrane 4a–l bearing 1H-pyrazole has been synthesized by one pot base catalyzed cyclocondensation reaction of 1H-pyrazole-4-carbaldehyde 1a–l, malononitrile 2 and 4-hydroxy-6-methylpyrone 3. All the synthesized compounds were screened against six bacterial pathogens, namely B. subtilis, C. tetani, S. pneumoniae, S. typhi, V. cholerae, E. coli and antifungal activity against, two fungal pathogens, A. fumigatus and C. albicans using broth microdilution MIC method. Some of the compounds are found to be equipotent or more potent than that of commercial drugs, against most of employed strains.

A new series of twenty four derivatives of pyrano[3,2-c]chromene IVa-x bearing 1H-pyrazole were synthesized by a one pot, base-catalyzed cyclocondensation reaction of 1H-pyrazole-4-carbaldehyde Ia-l, malononitrile II and 4-hydroxycoumarin IIIa-b. All the synthesized compounds were characterized by elemental analysis, FT-IR, 1H NMR and 13C NMR spectral data. All the synthesized compounds were screened against six bacterial pathogens, namely B. subtilis, C. tetani, S. pneumoniae, S. typhi, V. cholerae, E. coli and for antifungal activity against two fungal pathogens, A. fumigatus and C. albicans using the broth microdilution MIC method. Some of the compounds were found to be equipotent or more potent than commercial drugs against most of employed strains, as evident from the screening data.

Recently, various nanomaterials have been used in many organic transformations as efficient catalysts. The development of new catalysts by nanoscale design has emerged as a fertile field for research and innovation. The ability of nanotechnology to enhance catalytic activity opens the potential to replace expensive catalysts with lower amounts of inexpensive nanocatalysts. Besides, development of efficient and environmentally friendly synthetic methodologies for the synthesis of compound libraries of medicinal scaffolds is an attractive area of research in both academic and pharmaceutical industry. According to above reports and needs, this review deals with applications of nanoparticles as catalysts in various organic syntheses. We detail the topic of organic transformations using nanoparticles: Metal Nanoparticles and Metal Oxide Nanoparticles. In the latter part, different Metal Oxide Nanoparticles, such as ZnO Nanoparticle, TiO2 Nanoparticle, and CuO Nanoparticle are discussed.

Twenty eight 6,7-dihydrobenzo[f]benzo[4,5]imidazo[1,2-d][1,4]oxazepine derivatives were synthesized and evaluated their biological activities as PI3K inhibitors. Biological evaluation against four human tumor cell lines revealed that most target compounds showed impressively better antiproliferative activities than that of LY294002. Among these compounds, compound 25 exhibited the most potent and selective activity for PI3Kα, with the IC50 value of 0.016μM, an approximately 30-fold increase in comparison with LY294002, it also has an increased potency of approximately 11-fold for PI3Kβ. It indicated the potential of developing 6,7-dihydrobenzo[f]benzo[4,5]imidazo[1,2-d][1,4]oxazepine derivatives as the new PI3Kα selective inhibitors for tumor treatment.

Many reports implied that the BRAF serine/threonine kinase was mutated in various types of human tumors, which were related with cell growth, survival and differentiation. To provide new therapeutic opportunities, a series of novel 4,5-dihydro-1H-pyrazole derivatives (6a-10d) containing thiazole moiety as potential V600E mutant BRAF kinase (BRAF(V600E)) inhibitors were designed and synthesized. All compounds were evaluated in vitro for anticancer activities against WM266.4 human melanoma cell line and breast cancer MCF-7 cell line. Compound 10d displayed the most potential antiproliferative activity with an IC50 value of 0.12μM against cell line WM266.4 and 0.16μM against MCF-7 with positive control Sorafenib. Results of the inhibitory activity against BRAF(V600E) revealed that compound 10d was bearing the best bioactivity with IC50 of 0.05μM as well. On the basis of the result of flow cytometry, with the dose of compound 10d increasing, more and more cancer cell gradually encountered apoptosis or died, which indicated the compound 10d could induce remarkable apoptosis of MCF-7 and WM266.4 cells in a dose dependent manner. Furthermore, docking simulation of inhibitor analogues and 3D-QSAR modeling provided potential binding model and further knowledge of pharmacophore.

A new series of biquinoline-pyridine hybrids were designed and synthesized by a base-catalyzed cyclocondensation through one-pot multicomponent reaction. All compounds were tested for in vitro anticancer activities against two cancer cell lines A549 (adenocarcinomic human alveolar basal epithelial) and Hep G2 (liver cancer). Enzyme inhibitory activities of all compounds were carried out against EGFR and HER-2 kinase. Of the compounds studied, majority of the compounds showed effective anticancer activity against used cancer cell lines. Compound 9i (IC50=0.09 μM) against EGFR and (IC50=0.2 μM) against HER-2 kinase displayed the most potent inhibitory activity as compared to other member of the series. In the molecular modelling study, compound 9i was bound in to the active pocket of EGFR with four hydrogen bonds and two π-cation interactions having minimum binding energy ΔGb=-54.4 kcal/mol.

New Schiff’s base derivatives 5a–j have been synthesized by reaction between 2-phenoxyquinoline-3-carbaldehydes 3a–j and 2-(2-methyl-5-nitro-1H-imidazol-1-yl)acetohydrazide 4 in presence of nickel(II) nitrate as a catalyst in ethanol under reflux in good yield (78–92%). All compounds were tested for anticancer and inhibition of EGFR. Of the compounds studied, majority of the compounds showed effective antiproliferation and inhibition of EGFR and HER-2 activities. Compound 5h showed most effective inhibition (IC50 = 0.12 ± 0.05 μM) by binding in to the active pocket of EGFR receptor with minimum binding energy (ΔGb = −58.3691 kcal/mol). The binding was stabilized by two hydrogen bonds, two π–cation and one π–sigma interactions. Compound 5d showed most effective inhibition (IC50 = 0.37 ± 0.04 μM).