pubmed:abstractText |
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.
|
pubmed:affiliation |
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. Vassilios.Bavetsias@icr.ac.uk
|