Preparation of spermine conjugates with acidic retinoids with potent ribonuclease P inhibitory activity.
Novel mono- and diacylated spermines, readily obtained using isolable succinimidyl active esters of acidic retinoids for the selective acylation of free spermine or in situ activated acidic retinoids for acylating selectively protected spermine followed by deprotection, were shown to inhibit the ribozyme ribonuclease P more strongly than the parent retinoids.
Magoulas
George
G
Department of Chemistry, School of Natural Sciences, University of Patras, University Campus, GR-26504 Patras, Greece.
Papaioannou
Dionysios
D
Papadimou
Evangelia
E
Drainas
Denis
D
D000818:Animals; D004023:Dictyostelium / Q000166:cytology / Q000201:enzymology; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D043262:Ribonuclease P / Q000037:antagonists & inhibitors* / Q000302:isolation & purification; D013096:Spermine / Q000737:chemistry*; D013237:Stereoisomerism; D014212:Tretinoin / Q000031:analogs & derivatives / Q000737:chemistry / Q000494:pharmacology*
D004791:Enzyme Inhibitors; D013096:Spermine; D014212:Tretinoin; D043262:Ribonuclease P