title: Synthesis of aniline-type analogues of farnesyl diphosphate and their biological assays for prenyl protein transferase inhibitory activity.
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.
authors: Dipartimento di Scienze Farmaceutiche, Università di Pisa, Via Bonanno 6, 56126 Pisa, Italy.
authors: Filippo
authors: F
authors: Minutolo
authors: Simone
authors: S
authors: Bertini
authors: Laura
authors: L
authors: Betti
authors: Valeria
authors: V
authors: Di Bussolo
authors: Gino
authors: G
authors: Giannaccini
authors: Giorgio
authors: G
authors: Placanica
authors: Simona
authors: S
authors: Rapposelli
authors: H Peter
authors: HP
authors: Spielmann
authors: Marco
authors: M
authors: Macchia
mesh_terms: D000814:Aniline Compounds / Q000138:chemical synthesis* / Q000494:pharmacology; D001681:Biological Assay / Q000379:methods*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D011106:Polyisoprenyl Phosphates / Q000138:chemical synthesis* / Q000494:pharmacology; D011506:Proteins / Q000378:metabolism; D012717:Sesquiterpenes; D014166:Transferases / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D000814:Aniline Compounds; D004791:Enzyme Inhibitors; D011106:Polyisoprenyl Phosphates; D011506:Proteins; D012717:Sesquiterpenes; C004808:farnesyl pyrophosphate; D014166:Transferases