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

作者信息

Minutolo Filippo, Bertini Simone, Betti Laura, Di Bussolo Valeria, Giannaccini Gino, Placanica Giorgio, Rapposelli Simona, Spielmann H Peter, Macchia Marco

机构信息

Dipartimento di Scienze Farmaceutiche, Università di Pisa, Via Bonanno 6, 56126 Pisa, Italy.

出版信息

Farmaco. 2003 Dec;58(12):1277-81. doi: 10.1016/j.farmac.2003.08.002.

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.

摘要

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