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ID: ALA1139292

Journal: Bioorg Med Chem Lett

Title: Tetrahydroisoquinoline amide substituted phenyl pyrazoles as selective Bcl-2 inhibitors.

Authors: Porter J, Payne A, de Candole B, Ford D, Hutchinson B, Trevitt G, Turner J, Edwards C, Watkins C, Whitcombe I, Davis J, Stubberfield C.

Abstract: Anti-apoptotic Bcl-2 protects cells from apoptosis by binding to pro-apoptotic members of the Bcl-2 family thereby playing a role in tumour survival in response to chemo- or radiation therapy. We describe a series of phenyl pyrazoles that have high affinity for Bcl-2 and rationalise the observed SAR by means of an X-ray crystal structure.

CiteXplore: 19027294

DOI: 10.1016/j.bmcl.2008.10.113