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ID: ALA1136489

Journal: Bioorg Med Chem Lett

Title: Stable analogues of geranylgeranyl diphosphate possessing improved geranylgeranyl versus farnesyl protein transferase inhibitory selectivity.

Authors: Minutolo F, Bertini S, Betti L, Danesi R, Gervasi G, Giannaccini G, Papi C, Placanica G, Barontini S, Rapposelli S, Macchia M.

Abstract: Phosphonoacetamido(oxy) groups have proven to be good mimics of the diphosphate portion in geranylgeranyl protein transferase I (GGTase I) inhibitors. The introduction of small alkyl groups (Me, Et) into the diphosphate mimic moiety caused a further decrease in collateral farnesyl protein transferase (FTase) inhibitory activity, thereby improving GGTase I over FTase selectivity.

CiteXplore: 14643335

DOI: 10.1016/j.bmcl.2003.09.035