Synthesis and in vitro evaluation of novel isatinincorporated thiadiazole hybrids as potential anti-breast cancer agents
Purpose: To synthesis and characterize some novel isatin-incorporated thiadiazoles and screen them for anti-breast cancer activity in human breast adenocarcinoma cells (MCF-7).
Method: A series of isatin incorporated Schiff bases of thiadiazoles (3a-3l) was synthesized by reaction of substituted thiadiazoles (1a-1d) with isatin (2a) and N-alkyl substituted isatin (2b-2c) and characterized by elemental analysis, IR, 1H NMR, 13C NMR and LCMS. The newly synthesized compounds were screened for their in-vitro cytotoxicity against MCF-7 cell lines by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) colorimetric and Sulforhodamine B (SRB) methods.
Results: Compounds 3a, 3c, 3d, 3g and 3j showed anticancer activity in both MTT and SRB assay. Compound 3-(5-(4-chlorophenyl)-1,3,4-thiadiazol-2-ylimino)-1-ethylindolin-2-one (3g) showed most potent cytotoxic activity against MCF-7 cell lines.
Conclusion: The novel isatin incorporated thiadiazoles synthesized and characterized in this study possess anti-cancer activities in human breast adenocarcinoma cells (MCF-7). This can possibly lead to emergence of new anti-breast cancer agents.
Keywords: Thiadiazoles, Isatin, In-vitro cytotoxicity, Human breast adenocarcinoma cells (MCF-7), SRB assay
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