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Synthesis and biological evaluation of novel N-methyl-picolinamide-4-thiol derivatives as potential antitumor agents.

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.

SUBMITTER: Huang TT

PROVIDER: S-EPMC6268926 | biostudies-literature | 2012 May

REPOSITORIES: biostudies-literature

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Synthesis and biological evaluation of novel N-methyl-picolinamide-4-thiol derivatives as potential antitumor agents.

Huang Ting-Ting TT Huang Yun-Chuang YC Qing Xiao-Yu XY Xia Yong Y Luo Xun X Ye Ting-Hong TH Yu Luo-Ting LT

Molecules (Basel, Switzerland) 20120525 6

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 6 ...[more]

PMID: 22634842

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