LaBeaume Paul, Wager Krista, Falcone Danielle, Li Jane, Torchilin Vladimir, Castro Curtis, Holewa Coleen, Kallmerten Amy E, Jones Graham B
Department of Chemistry and Chemical Biology, Northeastern University, Boston, MA 02115, United States.
Bioorg Med Chem. 2009 Sep 1;17(17):6292-300. doi: 10.1016/j.bmc.2009.07.059. Epub 2009 Jul 26.
Methodology is outlined for the chemical synthesis of versatile photo-Bergman enediyne building blocks and their conjugates. Routes to both mono and bis conjugated enediyne templates are detailed together with representative examples of their bioconjugates, nanoconjugates, PEG derivatives and water soluble salts. The immunocompetence of antibody conjugates is retained, and application in the form of reagents for photodynamic therapy (PDT) advanced.
概述了用于化学合成多功能光伯格曼烯二炔结构单元及其共轭物的方法。详细介绍了单共轭和双共轭烯二炔模板的合成路线,以及它们的生物共轭物、纳米共轭物、聚乙二醇衍生物和水溶性盐的代表性实例。抗体共轭物的免疫活性得以保留,并推进了其作为光动力疗法(PDT)试剂形式的应用。