Synthesis and Biological Evaluation of Novel N-Methyl-picolinamide-4-thiol Derivatives as Potential Antitumor Agents

摘要

A novel series of N-methylpicolinamide-4-thiol derivatives were synthesized and evaluated on human cancer cell lines. Among them, compound >6p displayed potent and broad-spectrum anti-proliferative activities in vitro on some human cancer cell lines, even better than sorafenib. The advanced kinase inhibitory assays showed that compound >6p could selectively inhibit Aurora-B kinase. The biological results were rationalized by the molecular docking study, which indicated the stable interactions of >6p with the Aurora-B kinase.