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

Ting-Ting Huang, Yun-Chuang Huang, Xiao-Yu Qing, Yong Xia, Xun Luo, Ting-Hong Ye, Luo-Ting Yu
2012 Molecules  
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
more » ... le interactions of 6p with the Aurora-B kinase.
doi:10.3390/molecules17066317 pmid:22634842 fatcat:alrwrrvmvvevbai62kuawsfj24