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The Role of the Acidity of N-Heteroaryl Sulfonamides as Inhibitors of Bcl-2 Family Protein-Protein Interactions

Visser, Michael and Toure, Bakary-Barry and Porter, Dale and Herlihy, Kara and Perez, Lawrence and Springer, Clayton and Xie, Xiaoling (2013) The Role of the Acidity of N-Heteroaryl Sulfonamides as Inhibitors of Bcl-2 Family Protein-Protein Interactions. ACS Medicinal Chemistry Letters, 4 (2). pp. 186-190.

Abstract

Over expression of the antiapoptotic members of the Bcl-2 family of proteins is commonly associated with cancer cell survival and resistance to chemotherapeutics. Here we describe the structure-based optimization of a series of N-heteroaryl sulfonamides that demonstrate potent mechanism based cell death. The role of the acidic nature of the sulfonamide moiety as it relates to potency, solubility, and clearance is examined. This has led to the discovery of novel heterocyclic replacements for the acylsulfonamide core of ABT-737 and ABT-263.

Item Type: Article
Keywords: B Cell Lymphoma, Bcl-2 family, protein-protein interaction, apoptosis, cancer
Date Deposited: 26 Apr 2016 23:46
Last Modified: 26 Apr 2016 23:46
URI: https://oak.novartis.com/id/eprint/8253

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