Potent 2'-aminoanilide inhibitors of cFMS as potential anti-inflammatory agents |
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Authors: | Patch Raymond J Brandt Benjamin M Asgari Davoud Baindur Nand Chadha Naresh K Georgiadis Taxiarchis Cheung Wing S Petrounia Ioanna P Donatelli Robert R Chaikin Margery A Player Mark R |
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Institution: | Drug Discovery, Johnson and Johnson Pharmaceutical Research and Development, L.L.C., 8 Clarke Drive, Cranbury, NJ 08512, USA. |
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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. |
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