Synthesis and biological evaluation of 4-amino derivatives of benzimidazoquinoxaline, benzimidazoquinoline, and benzopyrazoloquinazoline as potent IKK inhibitors

被引：53
作者：
Beaulieu, Francis
Ouellet, Carl
Ruediger, Edward H.
Belema, Makonen
Qiu, Yuping
Yang, Xuejie
Banville, Jacques
Burke, James R.
Gregor, Kurt R.
MacMaster, John F.
Martel, Alain
McIntyre, Kim W.
Pattoli, Mark A.
Zusi, F. Christopher
Vyas, Dolatrai
机构：
[1] Bristol Myers Squibb Pharmaceut Res Inst, Candiac, PQ J5R 1J1, Canada
[2] Dept Discovery Chem, Wallingford, CT 06492 USA
[3] Dept Immunol Inflammat & Pulm Drug Discovery, Princeton, NJ 08543 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 05期
关键词：
NF-kappa B; IKK inhibitors; TNF-alpha; quinoxaline;
D O I：
10.1016/j.bmcl.2006.12.017
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
We have recently identified BMS-345541 (1) as a highly selective and potent inhibitor of IKK-2 (IC50 = 0.30 mu M), which however was considerably less potent against IKK-1 (IC50 = 4.0 mu M). 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. (c) 2006 Elsevier Ltd. All rights reserved.
引用
收藏
页码：1233 / 1237
页数：5
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