European Journal of Medicinal Chemistry 2015-01-01

Design and optimization of hybrid of 2,4-diaminopyrimidine and arylthiazole scaffold as anticancer cell proliferation and migration agents.

Wenbo Zhou, Anling Huang, Yong Zhang, Qingxiang Lin, Weikai Guo, Zihua You, Zhengfang Yi, Mingyao Liu, Yihua Chen

Index: Eur. J. Med. Chem. 96 , 269-80, (2015)

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Abstract

Therapeutics of metastatic or triple-negative breast cancer are still challenging in clinical. Herein we demonstrated the design and optimization of a series of hybrid of 2,4-diaminopyrimidine and arylthiazole derivatives for their anti-proliferative properties against two breast cancer cell lines (MCF-7 as human breast cancer and MDA-MB-231 as triple-negative breast cancer). More importantly, some of those compounds with potent antiproliferative activities also indicated excellent inhibitory activities against MDA-MB-231 cell migration. These results suggested that the new series of hybridation of aryl-thiazoles and aminopyrimidines could be identified and developed as novel highly potential anticancer agents against the triple-negative breast cancer as well as metastatic one in the future. Copyright © 2015 Elsevier Masson SAS. All rights reserved.