Synthesis Routes Towards the Farnesyl Protein Transferase Inhibitor ZARNESTRATM

…, MG Venet, W Filliers, R Broeckx…

Index: Angibaud, Patrick R.; Venet, Marc G.; Filliers, Walter; Broeckx, Rudy; Ligny, Yannick A.; Muller, Philippe; Poncelet, Virginie S.; End, Dave W. European Journal of Organic Chemistry, 2004 , # 3 p. 479 - 486

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Citation Number: 55

Abstract

Abstract The discovery that post-translational farnesylation of Ras oncoprotein was an essential step in exercising its biological effect led to the design of farnesyl protein transferase inhibitors (FTIs) in order to control growth of tumors bearing Ras mutations. Pre- clinical studies on murine models have confirmed their inhibitory effect on tumor growth and enabled clinical development. R115777 (ZARNESTRA TM) is currently undergoing ...