2. Academic Validation
  3. Synthesis and biological evaluation of 4-amino derivatives of benzimidazoquinoxaline, benzimidazoquinoline, and benzopyrazoloquinazoline as potent IKK inhibitors

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

  • Bioorg Med Chem Lett. 2007 Mar 1;17(5):1233-7. doi: 10.1016/j.bmcl.2006.12.017.
Francis Beaulieu 1,  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
Affiliations

Affiliation

  • 1 Bristol-Myers Squibb Pharmaceutical Research Institute, 100 boul. de l'Industrie, Candiac, Que., Canada J5R 1J1. [email protected]
PMID: 17197177 DOI: 10.1016/j.bmcl.2006.12.017
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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