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

Abstract

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

Keywords

• &lt;em&gt;N&lt;/em&gt;-methylpicolinamide-4-thiol derivatives
• antitumor
• Aurora-B kinase
• docking study