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

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
Type
Published Article
Journal
Bioorganic & Medicinal Chemistry Letters
Publisher
Elsevier
Publication Date
Mar 01, 2007
Volume
17
Issue
5
Pages
1233–1237
Identifiers
PMID: 17197177
Source
Medline
License
Unknown

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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