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

[ Vol. 3 , Issue. 10 ]


Marc Venet, David End and Patrick Angibaud   Pages 1095 - 1102 ( 8 )


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.


farnesyl protein transferase inhibition, zarnestra, r115777


Johnson&Johnson Pharmaceutical Research&Development L.L.C.3, Campus deMaigremont, BP 615, 27106 Val de Reuil Cedex, France

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