Identification of a phenylacylsulfonamide series of dual Bcl-2/Bcl-xL antagonists.
Basic Information
ID: ALA2029223
Journal: Bioorg Med Chem Lett
Title: Identification of a phenylacylsulfonamide series of dual Bcl-2/Bcl-xL antagonists.
Authors: Perez HL, Banfi P, Bertrand J, Cai ZW, Grebinski JW, Kim K, Lippy J, Modugno M, Naglich J, Schmidt RJ, Tebben A, Vianello P, Wei DD, Zhang L, Galvani A, Lombardo LJ, Borzilleri RM.
Abstract: 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.
CiteXplore: 22608961
DOI: 10.1016/j.bmcl.2012.04.103
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