A preparation of new series of 2'-hydrazinocholest-6-eno[4,5-d]thiazoles 4-6 from 5α-cholestan-6-ones 1-3 are herein reported. After
characterization by IR, 1H NMR, 13C NMR, MS and analytical data, the synthesized compounds 4-6 were tested for anticancer activity in
vitro against the human cancer cell lines A549, HepG2, HeLa, SW480 and HL-60 by MTT assay during which compounds 4-6 showed
significant anticancer behaviour. The gel electrophoresis pattern demonstrated that the compound 4 alone or in presence of Cu(II) causes
the nicking of super coiled pBR322. Further the compound 4 is also able to generate reactive oxygen species (hydroxyl radical) in a dose
dependent manner, which correlates its ability to cause DNA breakage in cancer cells. The genotoxicity of the compounds was studied by
comet assay involving potential apoptotic degradation of DNA and was analyzed by agarose gel electrophoresis and visualized by ethidium
bromide staining.
Key words: Thiazole; 5α-iodocholestan-6-one; MTT assay; pBR322; Comet assay.
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