Cell permeation of a Trypanosoma brucei aldolase inhibitor: evaluation of different enzyme-labile phosphate protecting groups

Bioorganic & Medicinal Chemistry Letters
Laurent AzémaCasimir Blonski

Abstract

A series of four prodrugs directed against Trypanosoma brucei aldolase bearing various transient enzyme-labile phosphate protecting groups was developed. Herein, we describe the synthesis and evaluation of cell permeation of these prodrugs. The oxymethyl derivative was the most efficient prodrug with a good recovering of the free drug (IC(50)=20 microM) and without any measurable cytotoxicity.

Citations

May 19, 2009·BMC Systems Biology·Seth B RobertsGregory A Buck
Sep 15, 2009·Molecular and Biochemical Parasitology·Ana Judith CáceresVéronique Hannaert
Jan 9, 2015·PLoS Neglected Tropical Diseases·Inês LoureiroJoana Tavares
Feb 2, 2008·Journal of Medicinal Chemistry·Scott J Hecker, Mark D Erion

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