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Synthesis and biological evaluation of 2,4-disubstituted thiazole amide derivatives as anticancer agent

Zhi-Hua Zhang, Hong-Mei Wu, Sai-Nan Deng, Rui-Xia Chai, Muriira Cyrus Mwenda, Yuan-Yuan Peng, Dong Cai, and Yu Chen

Liaoning University of Technology, Jinzhou, China

 

E-mail: Caidong0804@163.com

Abstract: A series of novel 2,4-disubstituted thiazole amide derivatives were synthesized, and their antiproliferative activities were tested. Some of these compounds displayed good antiproliferative activity, especially for HT29 cell. Among these compounds, compound 5b inhibits A549, HeLa, HT29 and Karpas299 cells with IC50 values of 8.64, 6.05, 0.63 and 13.87 μM, respectively. The western blot analysis and docking study provide important clues for further optimization of compound 5b as a potential c-Met inhibitor.

Keywords: Thiazole derivatives ; Synthesis ; Anticancer activity 

Full paper is available at www.springerlink.com.

DOI: 10.1007/s11696-018-0587-3

 

Chemical Papers 73 (2) 355–364 (2019)

Tuesday, April 16, 2024

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