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

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Patch RJ, Brandt BM, Asgari D, Baindur N, Chadha NK, Georgiadis T, Cheung WS, Petrounia IP, Donatelli RR, Chaikin MA, Player MR

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

Bioorg Med Chem Lett. 2007 Nov 15;17(22):6070-4. Epub 2007 Sep 19.

PubMed ID

17904845 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
5-CYANO-FURAN-2-CARBOXYLIC ACID [5-HYDROXYMETHYL-2-(4-METHYL-PIPERIDIN-1-YL)-PHENYL]-AMIDE	Macrophage colony-stimulating factor 1 receptor	IC 50 (nM)	24	N/A	N/A	Details
5-CYANO-FURAN-2-CARBOXYLIC ACID [5-HYDROXYMETHYL-2-(4-METHYL-PIPERIDIN-1-YL)-PHENYL]-AMIDE	Macrophage colony-stimulating factor 1 receptor	IC 50 (nM)	250	N/A	N/A	Details