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


Journal Article

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.

Full Text

Duke Authors

Cited Authors

  • Beaulieu, F; Ouellet, C; Ruediger, EH; Belema, M; Qiu, Y; Yang, X; Banville, J; Burke, JR; Gregor, KR; MacMaster, JF; Martel, A; McIntyre, KW; Pattoli, MA; Zusi, FC; Vyas, D

Published Date

  • March 1, 2007

Published In

Volume / Issue

  • 17 / 5

Start / End Page

  • 1233 - 1237

PubMed ID

  • 17197177

Pubmed Central ID

  • 17197177

International Standard Serial Number (ISSN)

  • 0960-894X

Digital Object Identifier (DOI)

  • 10.1016/j.bmcl.2006.12.017


  • eng

Conference Location

  • England