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学科主题: 生命有机化学
题名: Discovery and Development of Thiazolo[3,2-a]pyrimidinone Derivatives as General Inhibitors of Bcl-2 Family Proteins
其他题名: 噻唑并(3,2-α)嘧啶酮作为Bcl-2家族蛋白通用抑制剂的发现和发展
作者: Zhou BC(周炳城) ; Li X(李勋) ; Li Y(李嫣) ; Xu YC(许耀春) ; Zhang ZX(张征西) ; Zhou M(周蜜) ; Zhang XL(张兴龙) ; Liu Z(刘真) ; Zhou JH(周佳海) ; Cao CY(曹春阳) ; Yu B(俞飚) ; Wang RX(王任小)
通讯作者: 俞飚 ; 王任小
刊名: ChemMedChem
发表日期: 2011-01-01
卷: 6, 期:5, 页:904-921
收录类别: SCI
部门归属: 中科院上海有机化学研究所; 北京大学
英文摘要: 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 compound were guided by the outcomes of molecular modeling studies. Among the 42 compounds obtained, a number of them exhibited much improved binding affinities to Bcl-2 family proteins as compared to the lead compound. The most potent compound, BCL-LZH-40, inhibited the binding of BH3 peptides to Bcl-x(L), Bcl-2, and Mcl-1 with inhibition constants (K(i)) of 17, 534, and 200 nm, respectively.
语种: 英语
相关网址: 查看原文
WOS记录号: WOS:000289860900019
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内容类型: 期刊论文
URI标识: http://ir.sioc.ac.cn/handle/331003/19141
Appears in Collections:生命有机化学国家重点实验室_期刊论文

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Recommended Citation:
Zhou BC,Li X,Li Y,et al. Discovery and Development of Thiazolo[3,2-a]pyrimidinone Derivatives as General Inhibitors of Bcl-2 Family Proteins[J]. ChemMedChem,2011,6(5):904-921.
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