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

Molecules

Ting-Ting Huang¹  Yun-Chuang Huang¹  Xiao-Yu Qing¹  Yong Xia¹  Xun Luo¹  Ting-Hong Ye¹ 

[1] State Key Laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University, Chengdu 610041, China

关键词: N-methylpicolinamide-4-thiol derivatives;    antitumor;    Aurora-B kinase;    docking study;   

DOI  :  10.3390/molecules17066317

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.