2. Academic Validation
  3. 2-Alkylamino- and alkoxy-substituted 2-amino-1,3,4-oxadiazoles-O-Alkyl benzohydroxamate esters replacements retain the desired inhibition and selectivity against MEK (MAP ERK kinase)

2-Alkylamino- and alkoxy-substituted 2-amino-1,3,4-oxadiazoles-O-Alkyl benzohydroxamate esters replacements retain the desired inhibition and selectivity against MEK (MAP ERK kinase)

  • Bioorg Med Chem Lett. 2008 Dec 1;18(23):6171-4. doi: 10.1016/j.bmcl.2008.10.015.
Joseph S Warmus 1,  Cathlin Flamme,  Lu Yan Zhang,  Stephen Barrett,  Alexander Bridges,  Huifen Chen,  Richard Gowan,  Michael Kaufman,  Judy Sebolt-Leopold,  Wilbur Leopold,  Ronald Merriman,  Jeffrey Ohren,  Alexander Pavlovsky,  Sally Przybranowski,  Haile Tecle,  Heather Valik,  Christopher Whitehead,  Erli Zhang
Affiliations

Affiliation

  • 1 Department of Chemistry, Pfizer Global Research and Development, Ann Arbor, MI 48105, USA. Joseph.Warmus@Pfizer.com
PMID: 18951019 DOI: 10.1016/j.bmcl.2008.10.015
Abstract

This paper reports a second generation MEK Inhibitor. The previously reported potent and efficacious MEK Inhibitor, PD-184352 (CI-1040), contains an integral hydroxamate moiety. This compound suffered from less than ideal solubility and metabolic stability. An oxadiazole moiety behaves as a bioisostere for the hydroxamate group, leading to a more metabolically stable and efficacious MEK Inhibitor.

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