Preparation of spermine conjugates with acidic retinoids with potent ribonuclease P inhibitory activity

George Magoulas; Dionysios Papaioannou; Evangelia Papadimou; Denis Drainas

doi:10.1016/j.ejmech.2009.01.001

Preparation of spermine conjugates with acidic retinoids with potent ribonuclease P inhibitory activity

Eur J Med Chem. 2009 Jun;44(6):2689-95. doi: 10.1016/j.ejmech.2009.01.001. Epub 2009 Jan 19.

Authors

George Magoulas¹, Dionysios Papaioannou, Evangelia Papadimou, Denis Drainas

Affiliation

¹ Department of Chemistry, School of Natural Sciences, University of Patras, University Campus, GR-26504 Patras, Greece.

PMID: 19216007
DOI: 10.1016/j.ejmech.2009.01.001

Abstract

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Dictyostelium / cytology
Dictyostelium / enzymology
Dose-Response Relationship, Drug
Drug Design
Enzyme Inhibitors / chemical synthesis
Enzyme Inhibitors / chemistry
Enzyme Inhibitors / pharmacology*
Molecular Structure
Ribonuclease P / antagonists & inhibitors*
Ribonuclease P / isolation & purification
Spermine / chemistry*
Stereoisomerism
Tretinoin / analogs & derivatives
Tretinoin / chemistry
Tretinoin / pharmacology*

Substances

Enzyme Inhibitors
Spermine
Tretinoin
Ribonuclease P