Towards the next generation of dual Bcl-2/Bcl-x L inhibitors

…, P Mukherjee, JC Saeh, T MacIntyre, G Repik…

Index: Varnes, Jeffrey G.; Gero, Thomas; Huang, Shan; Diebold, R. Bruce; Ogoe, Claude; Grover, Paul T.; Su, Mei; Mukherjee, Prasenjit; Saeh, Jamal Carlos; Macintyre, Terry; Repik, Galina; Dillman, Keith; Byth, Kate; Russell, Daniel John; Ioannidis, Stephanos Bioorganic and Medicinal Chemistry Letters, 2014 , vol. 24, # 14 p. 3026 - 3033

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Abstract

Abstract Structural modifications of the left-hand side of compound 1 were identified which retained or improved potent binding to Bcl-2 and Bcl-x L in in vitro biochemical assays and had strong activity in an RS4; 11 apoptotic cellular assay. For example, sulfoxide diastereomer 13 maintained good binding affinity and comparable cellular potency to 1 while improving aqueous solubility. The corresponding diastereomer (14) was ...