Identification of potent type I MetAP inhibitors by simple bioisosteric replacement. Part 1: Synthesis and preliminary SAR studies of thiazole-4-carboxylic acid thiazol-2- …

YM Cui, QQ Huang, J Xu, LL Chen, JY Li, QZ Ye…

文献索引：Cui, Yong-Mei; Huang, Qing-Qing; Xu, Jie; Chen, Ling-Ling; Li, Jing-Ya; Ye, Qi-Zhuang; Li, Jia; Nan, Fa-Jun Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 16 p. 3732 - 3736

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被引用次数: 15

摘要

A series of thiazole-4-carboxylic acid thiazol-2-ylamide (TCAT, 4) derivatives were designed and synthesized according to simple bioisosteric replacement from previously reported pyridine-2-carboxylic acid thiazol-2-ylamide (PCAT) MetAP inhibitors. The preliminary SAR studies demonstrated that these TCAT series of compounds showed different activity and selectivity compared with those of the corresponding PCAT compounds. These findings ...