Design, synthesis and biological evaluation of some novel substituted 2-mercapto-3-phenethylquinazolines as antitumor agents

Abstract

A novel series of 2-(substituted thio)-3-phenethylquinazolin-4(3H)-one and 2-([5-mercapto-4-(substituted)-4H-1,2,4-triazol-3-yl)methylthio]-3-phenethylquinazolin-4(3H)-one (1–25) were designed, synthesized, and evaluated for their in vitro antitumor activity. A single dose (10 μM) of the test compounds was used in the National Cancer Institute (NCI) 60 cell lines panel assay. Compound 2 showed sensible selective activities toward renal and breast cancer cell lines, whereas breast cancer cell lines showed moderate sensitivity to compound 13. At the same time, compound 22 yielded reasonable selective activities toward leukemia and non-small cell lung cancer cell lines. The results achieved can be used as a useful template for future development and further derivatization or modification to obtain more potent and selective antitumor agents.