J. Med. Chem. 2010, 53, 6361–6367 6361 DOI: 10.1021/jm100487z
Nonpeptidic and Potent Small-Molecule Inhibitors of cIAP-1/2 and XIAP Proteins Haiying Sun,† Jianfeng Lu,† Liu Liu,† Han Yi,† Su Qiu,† Chao-Yie Yang,† Jeffrey R. Deschamps,‡ and Shaomeng Wang*,† †
Comprehensive Cancer Center and Departments of Internal Medicine, Pharmacology, and Medicinal Chemistry, University of Michigan, 1500 E. Medical Center Drive, Ann Arbor, Michigan 48109, and ‡Naval Research Laboratory, 4555 Overlook Avenue, Washington, D.C. 20375 Received April 20, 2010
A series of compounds were designed and synthesized as antagonists of cIAP-1/2 and XIAP based upon our previously identified lead compound SM-122 (1). The most potent of these (7) binds to XIAP, cIAP-1, and cIAP-2 proteins with Ki values of 36,
