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

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

State Key Laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University, Chengdu 610041, China
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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 (CC BY 3.0).

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MDPI and ACS Style

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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