2. Academic Validation
  3. Hit generation and exploration: imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases

Hit generation and exploration: imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases

  • Bioorg Med Chem Lett. 2007 Dec 1;17(23):6567-71. doi: 10.1016/j.bmcl.2007.09.076.
Vassilios Bavetsias 1,  Chongbo Sun,  Nathalie Bouloc,  Jóhannes Reynisson,  Paul Workman,  Spiros Linardopoulos,  Edward McDonald
Affiliations

Affiliation

  • 1 Department of Chemistry, Cancer Research UK Centre for Cancer Therapeutics, The Institute of Cancer Research, Cancer Research UK Laboratory, 15 Cotswold Road, Sutton, Surrey SM2 5NG, UK. [email protected]
PMID: 17933533 DOI: 10.1016/j.bmcl.2007.09.076
Abstract

A hit generation and exploration approach led to the discovery of 31 (2-(4-(6-chloro-2-(4-(dimethylamino)phenyl)-3H-imidazo[4,5-b]pyridin-7-yl)piperazin-1-yl)-N-(thiazol-2-yl)acetamide), a potent, novel inhibitor of Aurora-A, Aurora-B and Aurora-C kinases with IC(50) values of 0.042, 0.198 and 0.227microM, respectively. Compound 31 inhibits cell proliferation and has good microsomal stability.

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