2. Academic Validation
  3. Aryloxy substituted N-arylpiperazinones as dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I

Aryloxy substituted N-arylpiperazinones as dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I

  • Bioorg Med Chem Lett. 2001 Jun 4;11(11):1411-5. doi: 10.1016/s0960-894x(01)00240-2.
J M Bergman 1,  M T Abrams,  J P Davide,  I B Greenberg,  R G Robinson,  C A Buser,  H E Huber,  K S Koblan,  N E Kohl,  R B Lobell,  S L Graham,  G D Hartman,  T M Williams,  C J Dinsmore
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA.
PMID: 11378366 DOI: 10.1016/s0960-894x(01)00240-2
Abstract

A series of aryloxy substituted piperazinones with dual farnesyltransferase/geranylgeranyltransferase-I inhibitory activity was prepared. These compounds were found to have potent inhibitory activity in vitro and are promising agents for the inhibition of Ki-Ras signaling.

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