Synthesis of aniline-type analogues of farnesyl diphosphate and their biological assays for prenyl protein transferase inhibitory activity

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Abstract

Stable analogues of farnesyl diphosphate, possessing an aniline-type portion in the prenyl-mimic moiety and phosphonoacetamido(oxy) groups in the place of the metabolically unstable diphosphate unit, were synthesised and submitted to biological assays. The enzyme inhibition tests performed on FTase and GGTase I show that the newly synthesised compounds based on a combination of the aniline-containing portions with (phosphonoacetamido)oxy groups do not afford potent inhibitors. © 2003 Éditions scientifiques et médicales Elsevier SAS. All rights reserved.

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Minutolo, F., Bertini, S., Betti, L., Di Bussolo, V., Giannaccini, G., Placanica, G., … Macchia, M. (2003). Synthesis of aniline-type analogues of farnesyl diphosphate and their biological assays for prenyl protein transferase inhibitory activity. Farmaco, 58(12), 1277–1281. https://doi.org/10.1016/j.farmac.2003.08.002

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