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

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

Journal Name: Current Topics in Medicinal Chemistry

Volume 3 , Issue 10 , 2003

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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

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Article Details

Year: 2003
Page: [1095 - 1102]
Pages: 8
DOI: 10.2174/1568026033452050
Price: $58

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