Synthesis and Cytotoxicity Evaluation of Some Novel 1-(3-Chlorophenyl) piperazin-2-one Derivatives Bearing Imidazole Bioisosteres
摘要：
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.
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关键词：
FARNESYLTRANSFERASE INHIBITORS BIOLOGICAL EVALUATION ANTICANCER AGENTS COMPLEXES 3D-QSAR DESIGN SERIES DISCOVERY THIOUREA
DOI：
10.1071/CH13031
被引量：
年份：
2013
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