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5-(1H-Benzimidazol-1-yl)-3-alkoxy-2-thiophenecarbonitriles as potent, selective, inhibitors of IKK-epsilon kinase |
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| Authors: | Bamborough Paul Christopher John A Cutler Geoffrey J Dickson Marion C Mellor Geoffrey W Morey James V Patel Champa B Shewchuk Lisa M |
| Institution: | aGlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, UK bGlaxoSmithKline R&D, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK cGlaxoSmithKline Inc., 5 Moore Drive, Research Triangle Park, NC 27709, USA |
| Abstract: | The identification and hit-to-lead exploration of a novel, potent and selective series of substituted benzimidazole–thiophene carbonitrile inhibitors of IKK-ε kinase is described. Compound 12e was identified with an IKK-ε enzyme potency of pIC50 7.4, and has a highly encouraging wider selectivity profile, including selectivity within the IKK kinase family. |
| Keywords: | IKK-ε kinase inhibitors IKK |
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