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Bioorg Med Chem Lett. 2006 Nov 1;16(21):5561-6. Epub 2006 Aug 24.

Identification of isothiazole-4-carboxamidines derivatives as a novel class of allosteric MEK1 inhibitors.

Author information

1
Drug Discovery, Valeant Pharmaceutical Research and Development, 3300 Hyland Avenue, Costa Mesa, CA 92626, USA. HAbdellaoui@Cox.net

Abstract

The development of potent, orally bioavailable, and selective series of 5-amino-3-hydroxy-N(1-hydroxypropane-2-yl)isothiazole-4-carboxamidine inhibitors of MEK1 and MEK-2 kinase is described. Optimization of the carboxamidine and the phenoxyaniline group led to the identification of 55 which gave good potency as in vitro MEK1 inhibitors, and good oral exposure in rat.

PMID:
16934458
DOI:
10.1016/j.bmcl.2006.08.048
[Indexed for MEDLINE]

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