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ID: ALA1136216

Journal: Bioorg Med Chem Lett

Title: Potent quinoxaline-based inhibitors of PDGF receptor tyrosine kinase activity. Part 2: the synthesis and biological activities of RPR127963 an orally bioavailable inhibitor.

Authors: He W, Myers MR, Hanney B, Spada AP, Bilder G, Galzcinski H, Amin D, Needle S, Page K, Jayyosi Z, Perrone MH.

Abstract: RPR127963 demonstrates an excellent pharmacokinetic profile in several species and was found to be efficacious in the prevention of restenosis in a Yucatan mini-pig model upon oral administration of 1-5 mg/kg. The in vitro selectivity profile and SAR of the highly optimized PDGF-R tyrosine kinase inhibitor are highlighted.

CiteXplore: 12941342

DOI: 10.1016/s0960-894x(03)00655-3