Synthesis and biological evaluation of 4-amino derivatives of benzimidazoquinoxaline, benzimidazoquinoline, and benzopyrazoloquinazoline as potent IKK inhibitors |
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| Authors: | 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 |
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| Affiliation: | Bristol-Myers Squibb Pharmaceutical Research Institute, 100 boul. de l'Industrie, Candiac, Que., Canada J5R 1J1. francis.beaulieu@bms.com |
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| Abstract: | We have recently identified BMS-345541 (1) as a highly selective and potent inhibitor of IKK-2 (IC50 = 0.30 microM), which however was considerably less potent against IKK-1 (IC50 = 4.0 microM). 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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