Current Issue : October - December Volume : 2019 Issue Number : 4 Articles : 6 Articles
EGFR) dual inhibitors were designed and synthesized based on the structure of the\napproved EGFR inhibitor osimertinib (AZD9291). Among them, four compounds 5D, 5E, 9D and 9E\nexhibited more potent total HDAC inhibition than the approved HDAC inhibitor SAHA. However,\nthese compounds only showed moderate to low inhibitory potency towards EGFR with compounds\n5E and 9E possessing IC50 values against EGFR^WT and EGFRT^790M in the micromolar range.\n3-[4,5-dimethyl-2-thiazolyl]-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay revealed the potent\nantiproliferative activities of compounds 5D, 5E, 9D and 9E, among which 9E was even more\npotent against HeLa, MDA-MB-231, MDA-MB-468, HT-29 and KG-1 cell lines than SAHA and\nAZD9291. Further selectivity profile of 9E showed that this compound was not active against\nother 13 cancer-related kinases and two epigenetic targets lysine specific demethylase 1 (LSD1) and\nbromodomain-containing protein 4 (BRD4). These results support further structural modification of\n9E to improve its EGFR inhibitory activity, which will lead to more potent and balanced HDAC and\nEGFR dual inhibitors as anticancer agents....
A series of 3-amino-5-benzylphenol derivatives were designed and synthesized. Among\nthem, (3-benzyl-5-hydroxyphenyl)carbamates were found to exert good inhibitory activity against\nM. tuberculosis H37Ra, H37Rv and clinically isolated multidrug-resistant M. tuberculosis strains\n(MIC = 0.625â??6.25 microg/mL). The privileged compounds 3i and 3l showed moderate cytotoxicity against\ncell line A549. Compound 3l also exhibited potent in vivo inhibitory activity on a mouse infection\nmodel via the oral administration. The results demonstrated 3-hydroxyphenylcarbamates as a class\nof new antitubercular agents with good potential....
The sponge-derived fungus Penicillium sp. SCSIO41015 cultured on solid rice medium\nyielded twenty-one compounds (1-21), including two new alkaloids (1 and 2) and one new pyrone\nderivative (3). Their structures were elucidated by analysis of 1D/2DNMRdata and HR-ESI-MS. Their\nabsolute configurations were established by single-crystal X-ray diffraction analysis and comparison\nof the experimental with reported specific rotation values. Compound 16 exhibited selective cytotoxic\nactivity against the human gastric cancer cells MGC803, with IC^50 value of 5.19 microM. Compounds 9\nand 18 showed weak antibacterial activity against Staphylococcus aureus and Acinetobacter baumannii,\nrespectively, both with MIC values of 57 microg/mL. Furthermore, compound 16 displayed potent\nantibacterial activity against S. aureus with an MIC value of 3.75 microg/mL....
A novel flow-based approach for the preparation of benzimidazol-2-one (1) scaffold by the\n1,1â??-carbonyldiimidazole (CDI)-promoted cyclocarbonylation of o-phenylenediamine (2) is reported.\nStarting from a preliminary batch screening, the model reaction was successfully translated under\nflow conditions and optimised by means of design of experiment (DoE). The method allowed the\nefficient preparation of this privileged scaffold and to set up a general protocol for the multigram-scale\npreparation in high yield, purity, and productivity, and was successfully applied for the multigram flow\nsynthesis of N-(2-chlorobenzyl)-5-cyano-benzimidazol-2-one, which is a key synthon for hit-to-lead\nexplorations in our anti-inflammatory drug discovery program....
The development of the sustainable synthesis of zeolites has become a very hot topic in\nrecent years. Herein, we report a sustainable route for synthesizing all-silica SOD zeolite under\nsolvent-free conditions. The method of solvent-free synthesis includes mixing, grinding, and heating\nraw solids. The all-silica SOD zeolite obtained was well characterized by multiple measurement\ntechniques (XRD, SEM, IR, thermogravimetric-differential thermal analysis (TG-DTA), and magic\nangel spinning nuclear magnetic resonance (MAS NMR)). The crystallization process of all-silica\nSOD zeolite was also investigated in detail by XRD, SEM, UV-Raman, and MAS NMR techniques.\nIn addition, the effects of the crystallization compositions, including the molar ratios of Na2O/SiO2\nand ethylene glycol/SiO2, on the synthesis of the pure all-silica SOD zeolite were investigated at\ndifferent temperatures....
Synthesis and evaluation of ofloxacin derivatives were carried out and evaluated for their anthelmintic activity. Synthesized ofloxacin derivatives (Compounds 1-6) were purified by using of ethanol by recrystallization procedure and characterized the molecules by analytical methods (TLC), Spectroscopic methods (FT-IR, Mass and NMR). In-silico methods were adopted for synthetic derivatives by Molinspiration online software. Determined physicochemical parameters (In-silico studies) and bioactivity scores were noted for different derivatives. Evaluated anthelmintic activity of molecules of synthesized compounds by using mebendazole as standard drug. Equal concentrations of synthesized derivatives (30/50/100 mg/ml) by using DMSO solvent. Anthelmintic activity was achieved by Earthworms (Garg’s method)....
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