Farnesyl diphosphate-based inhibitors of Ras farnesyl protein transferase

…, EM Gordon, SS Robinson, V Manne

Index: Patel, Dinesh V.; Schmidt, Robert J.; Biller, Scott A.; Gordon, Eric M.; Robinson, Simon S.; Manne, Veeraswamy Journal of Medicinal Chemistry, 1995 , vol. 38, # 15 p. 2906 - 2921

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Citation Number: 98

Abstract

The rational design, synthesis, and biological activity of farnesyl diphosphate (FPP)-based inhibitors of the enzyme Ras farnesyl protein transferase (FPT) is described. Compound 3, wherein a, &carboxylic phosphonic acid type pyrophosphate (PPI surrogate is connected to the hydrophobic farnesyl group by an amide linker, was found to be a potent (150 (FPT)= 75 nM) and selective inhibitor of FPT, as evidenced by its inferior activity against squalene ...