Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1377992 | Bioorganic & Medicinal Chemistry Letters | 2007 | 5 Pages |
Abstract
We have recently identified BMS-345541 (1) as a highly selective and potent inhibitor of IKK-2 (IC50 = 0.30 μM), which however was considerably less potent against IKK-1 (IC50 = 4.0 μM). In order to further explore the SAR around the imidazoquinoxaline tricyclic structure of 1, we prepared a series of tetracyclic analogues (7, 13, and 18). The synthesis and biological activities of these potent IKK inhibitors are described.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Francis Beaulieu, Carl Ouellet, Edward H. Ruediger, Makonen Belema, Yuping Qiu, Xuejie Yang, Jacques Banville, James R. Burke, Kurt R. Gregor, John F. MacMaster, Alain Martel, Kim W. McIntyre, Mark A. Pattoli, F. Christopher Zusi, Dolatrai Vyas,