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Bioorg Med Chem Lett. 2004 Mar 22;14(6):1483-6.

Beyond U0126. Dianion chemistry leading to the rapid synthesis of a series of potent MEK inhibitors.

Author information

1
Bristol-Myers Squibb Pharmaceuticals Research Institute, PO Box 4000, Princeton, NJ 08543-4000, USA.

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.

PMID:
15006386
DOI:
10.1016/j.bmcl.2004.01.012
[Indexed for MEDLINE]

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