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

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

  • Eur J Med Chem. 2015:96:269-80. doi: 10.1016/j.ejmech.2015.04.027.
Wenbo Zhou 1 Anling Huang 1 Yong Zhang 1 Qingxiang Lin 1 Weikai Guo 1 Zihua You 1 Zhengfang Yi 1 Mingyao Liu 1 Yihua Chen 2
Affiliations

Affiliations

  • 1 Shanghai Key Laboratory of Regulatory Biology, The Institute of Biomedical Sciences and School of Life Sciences, East China Normal University, Shanghai, 200241, China.
  • 2 Shanghai Key Laboratory of Regulatory Biology, The Institute of Biomedical Sciences and School of Life Sciences, East China Normal University, Shanghai, 200241, China. Electronic address: yhchen@bio.ecnu.edu.cn.
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.

Keywords

Aminopyrimidines; Antitumor growth and metastasis; Arylthiazoles; Hybridation; Structure–activity relationships.

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