Hydroxamic acid-based bisubstrate analog inhibitors of Ras farnesyl protein transferase

…, MG Young, SP Robinson, L Hunihan…

Index: Patel, Dinesh V.; Young, Marian G.; Robinson, Simon P.; Hunihan, Lisa; Dean, Brenda J.; Gordon, Eric M. Journal of Medicinal Chemistry, 1996 , vol. 39, # 21 p. 4197 - 4210

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Citation Number: 41

Abstract

The rational design, synthesis, and activity of novel, hydroxamic acid-based, collective bisubstrate analog inhibitors of farnesyl protein transferase (FPT) is described. This class of compounds differ structurally from the conventional FPT inhibitors by being non-sulfhydryl and by being bisubstrate based rather than peptide or FPP derived inhibitors. Whereas replacement of the sulfhydryl group of tetrapeptide CVLS (I 50= 1 μM) by an N- ...