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

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; in revised form: 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

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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.

AMA 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(6):6317-6330.

Chicago/Turabian Style

Huang, Ting-Ting; Huang, Yun-Chuang; Qing, Xiao-Yu; Xia, Yong; Luo, Xun; Ye, Ting-Hong; Yu, Luo-Ting. 2012. "Synthesis and Biological Evaluation of Novel N-Methyl-picolinamide-4-thiol Derivatives as Potential Antitumor Agents." Molecules 17, no. 6: 6317-6330.

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