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ID: ALA1136215

Journal: Bioorg Med Chem Lett

Title: Potent quinoxaline-based inhibitors of PDGF receptor tyrosine kinase activity. Part 1: SAR exploration and effective bioisosteric replacement of a phenyl substituent.

Authors: Myers MR, He W, Hanney B, Setzer N, Maguire MP, Zulli A, Bilder G, Galzcinski H, Amin D, Needle S, Spada AP.

Abstract: Novel substituted 2-anilino- and 2-cycloalkylaminoquinoxalines have been found to be useful and selective inhibitors of PDGF-R autophosphorylation. Replacement of an anilino-substituent with substituted cyclohexylamino- or norbornylamino substituents led to significant improvements in the pharmacokinetic profile of these analogues.

CiteXplore: 12941341

DOI: 10.1016/s0960-894x(03)00654-1