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ID: ALA1158406
Journal: Bioorg Med Chem Lett
Title: Design of novel quinazoline derivatives and related analogues as potent and selective ALK5 inhibitors.
Authors: Gellibert F, Fouchet MH, Nguyen VL, Wang R, Krysa G, de Gouville AC, Huet S, Dodic N.
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 5mg/kg (bid).
CiteXplore: 19285388