Title of article
Cell permeation of a Trypanosoma brucei aldolase inhibitor: Evaluation of different enzyme-labile phosphate protecting groups
Author/Authors
Laurent Azéma، نويسنده , , Christian Lherbet، نويسنده , , Cécile Baudoin، نويسنده , , Casimir Blonski، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
4
From page
3440
To page
3443
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 (IC50 = 20 μM) and without any measurable cytotoxicity.
Keywords
Trypanosoma brucei , Aldolase , phosphate , Enzyme-labile protecting group , inhibitor , drug delivery
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2006
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
797007
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