2. Academic Validation
  3. Potent 2'-aminoanilide inhibitors of cFMS as potential anti-inflammatory agents

Potent 2'-aminoanilide inhibitors of cFMS as potential anti-inflammatory agents

  • Bioorg Med Chem Lett. 2007 Nov 15;17(22):6070-4. doi: 10.1016/j.bmcl.2007.09.057.
Raymond J Patch 1,  Benjamin M Brandt,  Davoud Asgari,  Nand Baindur,  Naresh K Chadha,  Taxiarchis Georgiadis,  Wing S Cheung,  Ioanna P Petrounia,  Robert R Donatelli,  Margery A Chaikin,  Mark R Player
Affiliations

Affiliation

  • 1 Drug Discovery, Johnson and Johnson Pharmaceutical Research and Development, L.L.C., 8 Clarke Drive, Cranbury, NJ 08512, USA.
PMID: 17904845 DOI: 10.1016/j.bmcl.2007.09.057
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.

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