Identification of a phenylacylsulfonamide series of dual Bcl-2/Bcl-xL antagonists

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• 作者：Heidi L. Perez^a ; ^{heidi.perez@bms.com} ; Patrizia Banfi^b ; Jay Bertrand^b ; Zhen-Wei Cai^a ; ^&dagger ; ; James W. Grebinski^a ; Kyoung Kim^a ; Jonathan Lippy^a ; Michele Modugno^b ; Joseph Naglich^a ; Robert J. Schmidt^a ; Andrew Tebben^a ; Paola Vianello^b ; ^&Dagger ; ; Donna D. Wei^a ; Liping Zhang^a ; Arturo Galvani^b ; Louis J. Lombardo^a ; ^§ ; ; Robert M. Borzilleri^a
• 关键词：Apoptosis ; Bcl-2 ; Bcl-xL ; Isolated mitochondria ; Protein&ndash ; protein interaction
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2012
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：15 June, 2012
• 卷：22
• 期：12
• 页码：3946-3950
• 文件大小：848 K

摘要

A series of phenylacylsulfonamides has been prepared as antagonists of Bcl-2/Bcl-xL. In addition to potent binding affinities for both Bcl-2 and Bcl-xL, these compounds were shown to induce classical markers of apoptosis in isolated mitochondria. Overall weak cellular potency was improved by the incorporation of polar functionality resulting in compounds with moderate antiproliferative activity.