Synthesis and Anticancer Activity of Novel Thiazole-5-Carboxamide Derivatives

Applied Sciences

Wen-Xi Cai⁴  Ai-Lin Liu¹  Zheng-Ming Li³  Wei-Li Dong⁴  Xing-Hai Liu⁵  Na-Bo Sun² 

[1] National Center for Pharmaceutical Screening, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China;College of Biology and Environmental Engineering, Zhejiang Shuren University, Hangzhou 310015, China;Collaborative Innovation Center of Chemical Science and Engineering, State Key Laboratory of Elemento-Organic Chemistry, Nankai University, Tianjin 300071, China;Tianjin Key Laboratory on Technologies Enabling Development of Clinical Therapeutics and Diagnostics (Theranostics), School of Pharmacy, Tianjin Medical University, Tianjin 300070, China;;College of Chemical Engineering, Zhejiang University of Technology, Hangzhou 310014, China

关键词: thiazole;    amide;    synthesis;    antitumour;   

DOI  :  10.3390/app6010008

来源: mdpi

【 摘 要 】

A series of novel 2-phenyl-4-trifluoromethyl thiazole-5-carboxamide derivatives have been synthesized and evaluated for their anticancer activity against A-549, Bel7402, and HCT-8 cell lines. Among the tested compounds, highest activity (48%) was achieved with the 4-chloro-2-methylphenyl amido substituted thiazole containing the 2-chlorophenyl group on the two position of the heterocyclic ring. Other structurally similar compounds displayed moderate activity. The key intermediates have been fully characterized.

【 授权许可】

CC BY   
© 2016 by the authors; licensee MDPI, Basel, Switzerland.