Shamsuzzaman, A. M. Dar, Hena Khanam
Sep 1, 2014
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Journal
Arabian Journal of Chemistry
Abstract
Abstract A series of new 5α-cholestano [5,6-b] benzothiazines ( 4 – 6 ) has been synthesized by the reaction of 5α-cholestan-6-one ( 1 – 3 ) with 2-aminothiophenol in the presence of iodine. The structures of newly synthesized compounds have been established on the basis of spectral and analytical data. Compounds ( 1 – 6 ) were screened for in vitro anticancer activity against the human cancer cell lines; SW480 (colon adenocarcinoma cells), A549 (lung carcinoma cells), HepG2 (hepatic carcinoma cells) and HeLa (cervical cancer cells) using MTT assay during which the products ( 4 – 6 ) showed marked increase in anticancer activity and in particular, compound 6 showed IC 50 = 13.73 μmol L −1 against HeLa cells, being more effective than Doxorubicin against the same cells. Compounds 4 and 6 also showed minimum IC 50 of 15.83 μmol L −1 and 16.89 μmol L −1 against HepG2 and A549 cells, respectively. Compounds ( 1 – 6 ) were also tested for in vitro antimicrobial activity against different bacterial as well as fungal strains during which newly synthesized compounds ( 4 – 6 ) were found more potent than starting compounds ( 1 – 3 ). Compound 4 was found to be more potent than the reference drug, Chloramphenicol, in the case of Escherichia coli while compound 5 was found almost equally potential antifungal agent against P. marneffei in comparison with the reference drug, Nystatin.