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ID: ALA1143306

Journal: Bioorg Med Chem Lett

Title: 3-amido-4-anilinoquinolines as CSF-1R kinase inhibitors 2: Optimization of the PK profile.

Authors: Scott DA, Bell KJ, Campbell CT, Cook DJ, Dakin LA, Del Valle DJ, Drew L, Gero TW, Hattersley MM, Omer CA, Tyurin B, Zheng X.

Abstract: The optimization of compounds from the 3-amido-4-anilinoquinolines series of CSF-1R kinase inhibitors is described. The series has excellent activity and kinase selectivity. Excellent physical properties and rodent PK profiles were achieved through the introduction of cyclic amines at the quinoline 6-position. Compounds with good activity in a mouse PD model measuring inhibition of pCSF-1R were identified.

CiteXplore: 19114305

DOI: 10.1016/j.bmcl.2008.12.044