Paper
Synthesis and antiproliferative evaluation of new (4-substituted-3,4-dihydro-2H-benzo[b][1,4]oxazin-2-yl)methane substituted sulfonamide derivatives
Published Dec 31, 2017 · Chandrakant Pawar, A. Sarkate, K. S. Karnik
European Journal of Chemistry
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Abstract
A series of new molecules having 4-substituted-3,4-dihydro-2 H -benzo[b][1,4]oxazin-2-yl)methane substituted sulfonamide derivatives were synthesized. The structures of the synthesized compounds were elucidated and confirmed by 1 H NMR, 13 C NMR, Mass spectra, and the purity was checked through HPLC analysis. The compounds were also evaluated for their in vitro antiproliferative activity against MCF-7, HeLa, A-549 and DU-145 cancer cell lines by MTT assay. Compounds 4d, 7c and 7d were tested for their activity against a panel of eight human kinase at 10 µM concentrations. Among them the compounds 4d and 7d showed very promising activity against CDK5/P25 kinase with 66 and 70% inhibitions, respectively. Compound 7c also showed promising activity of 59% inhibition. The preliminary bioassay showed that most of the compounds were antiproliferative with different degrees, and some compounds showed better activity than 5-fluorouracil which was used as positive control.
In Vitro StudyNew (4-substituted-3,4-dihydro-2H-benzo[b][1,4]oxazin-2-yl) methane substituted sulfonamide derivatives show promising antiproliferative activity against various cancer cell lines, with some showing better activity than
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