Farnesyl Protein Transferase Inhibitor ZARNESTRA™ R115777 - History of a Discovery

Title: Farnesyl Protein Transferase Inhibitor ZARNESTRA™ R115777 - History of a Discovery

Volume: 3 Issue: 10

Author(s): Marc Venet, David End and Patrick Angibaud

Affiliation:

Keywords: farnesyl protein transferase inhibition, zarnestra, r115777

Abstract: R115777 (R)-6-amino[(4-chlorophenyl)(1-methyl-1H-imidazol-5-yl)methyl]-4-(3-chlorophenyl)-1- methyl-2(1H)-quinolinone is a potent and selective inhibitor of farnesyl protein transferase with significant antitumor effects in vivo subsequent to oral administration in mice. Taking its roots into Janssens ketoconazole and retinoic acid catabolism programs, our interest into Ras prenylation process led us stepwise to identify the key structural features of R115777. Methodology, structure activity relationships, and pharmacology will be presented. R115777 is currently in phase III clinical evaluation.

Cite this article as:

Venet Marc, End David and Angibaud Patrick, Farnesyl Protein Transferase Inhibitor ZARNESTRA™ R115777 - History of a Discovery, Current Topics in Medicinal Chemistry 2003; 3 (10) . https://dx.doi.org/10.2174/1568026033452050