Discovery of novel c-Met kinase inhibitors bearing a thieno [2, 3-d] pyrimidine or furo [2, 3-d] pyrimidine scaffold

A Zhao, X Gao, Y Wang, J Ai, Y Wang, Y Chen…

文献索引：Zhao, Ailing; Gao, Xin; Wang, Yuanxiang; Ai, Jing; Wang, Ying; Chen, Yi; Geng, Meiyu; Zhang, Ao Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 13 p. 3906 - 3918

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被引用次数: 26

摘要

Abstract A series of thieno [2, 3-d] pyrimidines and furo [2, 3-d] pyrimidines were synthesized and evaluated for the c-Met inhibition. Thieno [2, 3-d] pyrimidine 6b stood out as the most potent showing an IC 50 of 35.7 nM. This compound displayed high inhibitory effect on cell proliferation in BaF3-TPR-Met cells and showed high selectivity for c-Met family against other 14 tested kinases. However, compound 6b was found ineffective in the c-Met- ...