Synthesis and biological evaluation of 2,4-disubstituted thiazole amide derivatives as anticancer agent
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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.
KeywordsThiazole derivatives Synthesis Anticancer activity
This work was supported by the National Natural Science Foundation of China (No. 21601075), the Natural Science Foundation of Liaoning Province (Nos. 2015020249, 20170540396) and General Research Projects of Liaoning Provincial Department of Education (No. JQL201715410).
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