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.

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

MINUTOLO, FILIPPO;BERTINI, SIMONE;BETTI, LAURA;DI BUSSOLO, VALERIA;GIANNACCINI, GINO;PLACANICA, GIORGIO;RAPPOSELLI, SIMONA;MACCHIA, MARCO
2003

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.
Minutolo, Filippo; Bertini, Simone; Betti, Laura; DI BUSSOLO, Valeria; Giannaccini, Gino; Placanica, Giorgio; Rapposelli, Simona; H. P., Spielmann; Macchia, Marco
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11568/184352
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