ISSN print edition: 0366-6352
ISSN electronic edition: 1336-9075
Registr. No.: MK SR 9/7
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
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.
Chemical Papers 73 (2) 355–364 (2019)