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Molecules 2012, 17(6), 6317-6330; doi:10.3390/molecules17066317
Article

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

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State Key Laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University, Chengdu 610041, China
* Author to whom correspondence should be addressed.
Received: 16 March 2012 / Revised: 3 May 2012 / Accepted: 17 May 2012 / Published: 25 May 2012
(This article belongs to the Section Medicinal Chemistry)
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Abstract

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.
Keywords: N-methylpicolinamide-4-thiol derivatives; antitumor; Aurora-B kinase; docking study N-methylpicolinamide-4-thiol derivatives; antitumor; Aurora-B kinase; docking study
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Huang, T.-T.; Huang, Y.-C.; Qing, X.-Y.; Xia, Y.; Luo, X.; Ye, T.-H.; Yu, L.-T. Synthesis and Biological Evaluation of Novel N-Methyl-picolinamide-4-thiol Derivatives as Potential Antitumor Agents. Molecules 2012, 17, 6317-6330.

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