Discovery of an orally bioavailable small molecule inhibitor of prosurvival B-cell lymphoma 2 proteins

…, H Ding, A Kunzer, KC Marsh, P Nimmer…

Index: Park, Cheol-Min; Oie, Tetsuro; Petros, Andrew M.; Zhang, Haichao; Nimmer, Paul M.; Henry, Rodger F.; Elmore, Steven W. Journal of the American Chemical Society, 2006 , vol. 128, # 50 p. 16206 - 16212

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Citation Number: 203

Abstract

Overexpression of prosurvival proteins such as Bcl-2 and Bcl-XL has been correlated with tumorigenesis and resistance to chemotherapy, and thus, the development of antagonists of these proteins may provide a novel means for the treatment of cancer. We recently described the discovery of 1 (ABT-737), which binds Bcl-2, Bcl-XL, and Bcl-w with high affinity, shows robust antitumor activity in murine tumor xenograft models, but is not orally ...