Design of novel quinazoline derivatives and related analogues as potent and selective ALK5 inhibitors |
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| Authors: | F. Gellibert M.-H. Fouchet V.-L. Nguyen R. Wang G. Krysa A.-C. de Gouville S. Huet N. Dodic |
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| Affiliation: | 1. GlaxoSmithKline, 25-27 Avenue du Québec, 91951 Les Ulis, France;2. GlaxoSmithKline, Research Triangle Park, NC 27703, USA |
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| Abstract: | Starting from quinazoline 3a, we designed potent and selective ALK5 inhibitors over p38MAP kinase from a rational drug design approach based on co-crystal structures in the human ALK5 kinase domain. The quinazoline 3d exhibited also in vivo activity in an acute rat model of DMN-induced liver fibrosis when administered orally at 5 mg/kg (bid). |
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