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
  • 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.