Discovery and Development of Thiazolo [3, 2??a] pyrimidinone Derivatives as General Inhibitors of Bcl??2 Family Proteins

…, X Zhang, Z Liu, J Zhou, C Cao, B Yu, R Wang

文献索引：Zhou, Bingcheng; Li, Xun; Li, Yan; Xu, Yaochun; Zhang, Zhengxi; Zhou, Mi; Zhang, Xinglong; Liu, Zhen; Zhou, Jiahai; Cao, Chunyang; Yu, Biao; Wang, Renxiao ChemMedChem, 2011 , vol. 6, # 5 p. 904 - 921

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被引用次数: 23

摘要

Abstract A class of compounds with a common thiazolo [3, 2-a] pyrimidinone motif has been developed as general inhibitors of Bcl-2 family proteins. The lead compound was originally identified in a random screening of a small compound library using a fluorescence polarization-based competitive binding assay. Its binding to the Bcl-x L protein was further confirmed by 15 N-HSQC NMR experiments. Structural modifications on the lead ...