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ID: ALA1140541
Journal: Bioorg Med Chem Lett
Title: Potent 2'-aminoanilide inhibitors of cFMS as potential anti-inflammatory agents.
Authors: Patch RJ, Brandt BM, Asgari D, Baindur N, Chadha NK, Georgiadis T, Cheung WS, Petrounia IP, Donatelli RR, Chaikin MA, Player MR.
Abstract: A series of 2'-aminoanilides have been identified which exhibit potent and selective inhibitory activity against the cFMS tyrosine kinase. Initial SAR studies within this series are described which examine aroyl and amino group substitutions, as well as the introduction of hydrophilic substituents on the benzene core. Compound 47 inhibits the isolated enzyme (IC(50)=0.027 microM) and blocks CSF-1-induced proliferation of bone marrow-derived macrophages (IC(50)=0.11 microM) and as such, serves as a lead candidate for further optimization studies.
CiteXplore: 17904845