Novel triazole based inhibitors of Ras farnesyl transferase

Ashis K Saha; Li Liu; Richard Simoneaux; Bart DeCorte; Christophe Meyer; Stacy Skrzat; Henry J Breslin; Michael J Kukla; Dave W End

doi:10.1016/j.bmcl.2005.09.007

Novel triazole based inhibitors of Ras farnesyl transferase

Bioorg Med Chem Lett. 2005 Dec 15;15(24):5407-11. doi: 10.1016/j.bmcl.2005.09.007. Epub 2005 Oct 10.

Authors

Ashis K Saha¹, Li Liu, Richard Simoneaux, Bart DeCorte, Christophe Meyer, Stacy Skrzat, Henry J Breslin, Michael J Kukla, Dave W End

Affiliation

¹ Department of Medicinal Chemistry, Janssen Research Foundation, Johnson & Johnson Pharmaceutical Research & Development, Welsh and McKean Roads, Spring House, PA 19477, USA. asaha@predixpharm.com

PMID: 16216509
DOI: 10.1016/j.bmcl.2005.09.007

Abstract

A novel series of potent inhibitors of Ras farnesyl transferase possessing a 1,2,4-triazole pharmacophore is described. These inhibitors were discovered from a parallel synthesis effort and were subsequently optimized to in vitro IC(50) value of less than 1nM.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Amino Acid Sequence
Enzyme Inhibitors / chemical synthesis*
Enzyme Inhibitors / pharmacology
Farnesyltranstransferase / antagonists & inhibitors*
Farnesyltranstransferase / genetics
Genes, ras
Models, Molecular
Molecular Conformation
Oligopeptides / chemistry
Triazoles / chemical synthesis*
Triazoles / pharmacology

Substances

Enzyme Inhibitors
Oligopeptides
Triazoles
Farnesyltranstransferase