title: Recent developments in the discovery of protein kinase inhibitors from the urea class.
abstract: With two compounds on the market (Gleevec and Iressa), and a number of drug candidates in late-stage clinical trials, small-molecule kinase inhibitors hold great potential as novel therapies for cancer and inflammatory disorders. Inhibitors from the urea class were first reported in 1996 and have emerged as an important compound class for medicinal chemists due to their unique binding mode and kinase inhibition profile. Currently, five members of this class are undergoing clinical trials, BIRB-796 (Boehringer Ingelheim Pharmaceuticals Inc), BAY-43-9006 (Bayer AG/Onyx Pharmaceuticals Inc), CP-547632 (Pfizer Inc), MLN-518 (Millennium Pharmaceuticals Inc) and KRN-951 (Kirin Brewery Co Ltd). This review focuses on the most recent developments in the discovery of urea-based protein kinase inhibitors.
authors.affiliation: Bayer Research Center, Bayer Pharmaceutical Corporation, West Haven, CT 06516, USA. jacques.dumas.b@bayer.com
authors.forename: Jacques
authors.initials: J
authors.lastname: Dumas
authors.forename: Roger A
authors.initials: RA
authors.lastname: Smith
authors.forename: Timothy B
authors.initials: TB
authors.lastname: Lowinger
mesh_terms: D002626:Chemistry, Pharmaceutical / Q000379:methods* / Q000639:trends; D017322:Clinical Trials, Phase II as Topic; D017326:Clinical Trials, Phase III as Topic; D015195:Drug Design; D006801:Humans; D015394:Molecular Structure; D009369:Neoplasms / Q000188:drug therapy; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D014508:Urea / Q000031:analogs & derivatives* / Q000737:chemistry / Q000627:therapeutic use
chemical_list: D047428:Protein Kinase Inhibitors; D014508:Urea