| Literature DB >> 15006386 |
John Wityak1, Frank W Hobbs, Daniel S Gardner, Joseph B Santella, Joseph J Petraitis, Jung-Hui Sun, Margaret F Favata, Andrea J Daulerio, Kurumi Y Horiuchi, Robert A Copeland, Peggy A Scherle, Bruce D Jaffe, James M Trzaskos, Ronald L Magolda, George L Trainor, John V Duncia.
Abstract
Employing phenylmalonitrile dianion chemistry, a large number of analogues of MEK inhibitor lead SH053 (IC(50)=140 nM) were rapidly synthesized leading to single digit nM inhibitors, displaying submicromolar AP-1 transcription inhibition in COS-7 cells. Compound 41, exhibiting a MEK IC(50)=12 nM showed ip activity in a TPA-induced ear edema model with an ED(50)=5 mg/kg.Entities:
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Year: 2004 PMID： 15006386 DOI： 10.1016/j.bmcl.2004.01.012
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823