2. Academic Validation
  3. Macrocyclic piperazinones as potent dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I

Macrocyclic piperazinones as potent dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I

  • Bioorg Med Chem Lett. 2004 Feb 9;14(3):639-43. doi: 10.1016/j.bmcl.2003.11.051.
Christopher J Dinsmore 1,  C Blair Zartman,  Jeffrey M Bergman,  Marc T Abrams,  Carolyn A Buser,  J Christopher Culberson,  Joseph P Davide,  Michelle Ellis-Hutchings,  Christine Fernandes,  Samuel L Graham,  George D Hartman,  Hans E Huber,  Robert B Lobell,  Scott D Mosser,  Ronald G Robinson,  Theresa M Williams
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA. [email protected]
PMID: 14741259 DOI: 10.1016/j.bmcl.2003.11.051
Abstract

A series of macrocyclic piperazinone compounds with dual farnesyltransferase/geranylgeranyltransferase-I inhibitory activity was prepared. These compounds were found to be potent inhibitors of protein prenylation in Cell Culture. A hypothesis for the binding mode of compound 3o in FPTase is proposed.

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