Synthesis and cytotoxicity evaluation of some novel 1-(3-Chlorophenyl) piperazin-2-one derivatives bearing imidazole bioisosteres

Abstract

A series of substituted 3-chlorophenylpiperazinone derivatives were synthesised using L-778123 (an imidazole-containing FTase inhibitor) as a model by bioisosteric replacement of the imidazole ring. The final compounds were evaluated against two human cancer cell lines including A549 (lung cancer) and HT-29 (colon cancer) by MTT assay. The results showed that substitution of imidazole ring with 1-amidinourea, semicarbazide, and thiobiuret led to improvement of cytotoxic activity against both cell lines. © 2013 CSIRO.