Guiraud Mathis, Ali Lamiaa M A, Gabrieli-Magot Emma, Lichon Laure, Daurat Morgane, Egron David, Gary-Bobo Magali, Peyrottes Suzanne
Team Nucleosides & Phosphorylated Effectors, IBMM, Pole Balard Recherche, University of Montpellier, CNRS, ENSCM, 34293 Montpellier, France.
Team Glyco & Nanovectors for Therapeutic Targeting, IBMM, Pole Balard Recherche, University of Montpellier, CNRS, ENSCM, 34293 Montpellier, France.
ACS Med Chem Lett. 2024 Feb 15;15(3):418-422. doi: 10.1021/acsmedchemlett.3c00568. eCollection 2024 Mar 14.
Herein, we report the design, the synthesis, and the study of novel triphenyl phosphonium-based nucleoside conjugates. 2'-Deoxycytidine was chosen as nucleosidic cargo, as it allows the introduction of fluorescein on the exocyclic amine of the nucleobase and grafting of the vector was envisaged through the formation of a biolabile ester bond with the hydroxyl function at the 5'-position. Compound was identified as a potential nucleoside prodrug, showing ability to be internalized efficiently into cells and to be co-localized with mitochondria.
在此,我们报告了新型三苯基鏻基核苷缀合物的设计、合成及研究。选择2'-脱氧胞苷作为核苷载体,因为它允许在核苷酸碱基的环外胺上引入荧光素,并且设想通过与5'-位羟基形成生物可裂解酯键来连接载体。化合物被鉴定为一种潜在的核苷前药,显示出能够有效内化进入细胞并与线粒体共定位的能力。