Azéma Laurent, Lherbet Christian, Baudoin Cécile, Blonski Casimir
Laboratoire SPCMIB, Groupe de Chimie Organique Biologique, Université Paul Sabatier UMR CNRS 5068, 118 route de Narbonne, 31062 Toulouse Cedex 4, France.
Bioorg Med Chem Lett. 2006 Jul 1;16(13):3440-3. doi: 10.1016/j.bmcl.2006.04.010. Epub 2006 Apr 24.
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.
开发了一系列四种针对布氏锥虫醛缩酶的前药，它们带有各种不稳定的酶促磷酸保护基团。在此，我们描述了这些前药的合成及其细胞渗透评估。氧甲基衍生物是最有效的前药，游离药物回收率良好（IC(50)=20 microM）且无任何可测细胞毒性。
