Guminski Yves, Grousseaud Martial, Cugnasse Sandrine, Brel Viviane, Annereau Jean-Philippe, Vispé Stéphane, Guilbaud Nicolas, Barret Jean-Marc, Bailly Christian, Imbert Thierry
Division de Chimie Médicinale, Centre de Recherche Pierre Fabre, 17 rue Jean Moulin, 81106 Castres cedex, France.
Bioorg Med Chem Lett. 2009 May 1;19(9):2474-7. doi: 10.1016/j.bmcl.2009.03.052. Epub 2009 Mar 18.
The synthesis of a series of conjugated spermine derivatives with benzoxadiazole, phenylxanthene or bodipy fluorophores is described. These fluorescent probes were used to identify the activity of the polyamine transport system (PTS). N(1)-Methylspermine NBD conjugate 5 proved to have the optimal fluorescence characteristics and was used to show a selectivity for PTS-proficient CHO versus PTS-deficient CHO-MG cells. It can therefore be used as a tool for the selection of cells sensitive to cytotoxic compounds vectored through the PTS.
本文描述了一系列带有苯并恶二唑、苯基呫吨或硼二吡咯荧光团的共轭精胺衍生物的合成。这些荧光探针用于鉴定多胺转运系统（PTS）的活性。N(1)-甲基精胺NBD共轭物5被证明具有最佳的荧光特性，并用于显示PTS功能正常的CHO细胞与PTS缺陷的CHO-MG细胞之间的选择性。因此，它可作为一种工具，用于筛选对通过PTS介导的细胞毒性化合物敏感的细胞。
