Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families.
Basic Information
ID: ALA2021801
Journal: Bioorg Med Chem Lett
Title: Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families.
Authors: Curtin ML, Frey RR, Heyman HR, Soni NB, Marcotte PA, Pease LJ, Glaser KB, Magoc TJ, Tapang P, Albert DH, Osterling DJ, Olson AM, Bouska JJ, Guan Z, Preusser LC, Polakowski JS, Stewart KD, Tse C, Davidsen SK, Michaelides MR.
Abstract: In an effort to identify multi-targeted kinase inhibitors with a novel spectrum of kinase activity, a screen of Abbott proprietary KDR inhibitors against a broad panel of kinases was conducted and revealed a series of thienopyridine ureas with promising activity against the Aurora kinases. Modification of the diphenyl urea and C7 moiety of these compounds provided potent inhibitors with good pharmacokinetic profiles that were efficacious in mouse tumor models after oral dosing. Compound 2 (ABT-348) of this series is currently undergoing Phase I clinical trials in solid and hematological cancer populations.
CiteXplore: 22465635
DOI: 10.1016/j.bmcl.2012.03.035
Patent ID: ┄