期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 4, 期 2, 页码 186-190出版社
AMER CHEMICAL SOC
DOI: 10.1021/ml300321d
关键词
B cell lymphoma; Bcl-2 family; protein-protein interaction; apoptosis; cancer
Overexpression 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.
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