Current Issue : January - March Volume : 2020 Issue Number : 1 Articles : 5 Articles
The compound 3-{[(2,3-Dichlorophenyl)amino]methyl}-5-(furan-2-ylmethylidene)-1,3-\nthiazolidine-2,4-dione has been designed, synthesized, and screened for its in vitro antibreast\ncancer activity, using human breast adenocarcinoma cell lines (MCF-7) and in vitro anti-inflammatory\nactivity. By hemolysis assay, it showed that it has a nonhemolytic and nontoxic effect on human blood\ncell. The title compound 5, subjected to in vitro activities, showed that it is cytotoxic with an IC50 of\n42.30 microM and a good anti-inflammatory agent. The docking results against cyclin dependent kinase 2\n(CDK2) (PDB ID: 3QQK) gave insights on its inhibitory activity...
Candida is a genus of yeasts and is the most common cause of fungal infections worldwide.\nHowever, only a few antifungal drugs are currently available for the treatment of Candida infections.\nIn the last decade, terpenophenols have attracted much attention because they often possess a\nvariety of biological activities. In the search for new antifungals, eight carveoylphenols were\nsynthesized and characterized by spectroscopic analysis. By using the broth microdilution assay,\nthe compounds were evaluated for antifungal activities in vitro against four human pathogenic yeast,\nand structure-activity relationships (SAR) were derived. Noteworthy, in this preliminary study,\ncompounds 5 and 6, have shown a significant reduction in the growth of all Candida strains tested.\nStarting from these preliminary results, we have designed the second generation of analogous in this\nclass, and further studies are in progress in our laboratories....
Three series of novel thienopyrimidine derivatives 9aâ??l, 15aâ??l, and 18aâ??h were designed\nand synthesized, and their IC50 values against four cancer cell lines HepG-2, A549, PC-3, and MCF-7\nwere evaluated. Most compounds show moderate cytotoxicity against the tested cancer cell lines.\nThe most promising compound 9a showed moderate activity with IC50 valuesâ?¦â?¦â?¦â?¦â?¦â?¦...
We designed and synthesized a series of novel 3-arylquinoxaline derivatives and evaluated\ntheir biological activities as potential dengue virus (DENV) replication inhibitors. Among them,\n[3-(4-methoxyphenyl)quinoxalin-2-yl](phenyl)methanol (19a), [6,7-dichloro-3-(4-methoxyphenyl)quinoxalin-\n2-yl](phenyl)methanol (20a), and (4-methoxyphenyl)(3-phenylquinoxalin-2-yl)methanone (21b) were found\nto significantly inhibit the DENV RNA expression in Huh-7-DV-Fluc cells with a potency better than that of\nribavirin. Compound 19a reduced DENV replication in both viral protein and messenger RNA (mRNA)\nlevels in a dose-dependent manner and exhibited no significant cell cytotoxicity. Notably, compound 19a\nexhibited a half maximal effective concentration (EC50) value������...
Reactive impurities, such as hydrogen peroxide in excipients, raise a great concern over the\nchemical stability of pharmaceutical products. Traditional screening methods of spiking impurities\ninto solid drug-excipient mixtures oversimplify the micro-environment and the physical state of\nsuch impurities in real dosage form. This can lead to an inaccurate prediction of the long-term\nproduct stability. This study presents the feasibility of using a polyvinylpyrrolidone-hydrogen\nperoxide complex (PVP-H2O2) as an oxidative agent for the solid state forced degradation of a\nselected drug, vortioxetine HBr. The PVP-H2O2 complex was prepared and characterized using\nFT-IR spectroscopy. The tablet compacts were made using a mixture of solid PVP-H2O2 complex\nand crystalline vortioxetine HBr powder. The compacts were exposed to 40 DegreeC/75% RH condition\nin open and closed states for different time intervals. The extent and the type of drug degradation\nwere analysed using LC and LC-MS. The extent of degradation was higher in the samples stored at\nthe open state as compared to the close state. The solution state forced oxidation was conducted to\nverify the peroxide induced degradation reactions. The results evidence the utility of the proposed\nsolid-state stressor and the method for screening the sensitivity of drugs to the excipient reactive\nimpurities involving peroxides in solid-state....
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