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.
Keywords: farnesyl protein transferase inhibition, zarnestra, r115777
Current Topics in Medicinal Chemistry
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.
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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
DOI https://dx.doi.org/10.2174/1568026033452050 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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