Article ID Journal Published Year Pages File Type
1377317 Bioorganic & Medicinal Chemistry Letters 2008 4 Pages PDF
Abstract

Efficient syntheses of a series of functionalized aryl enediynes have been developed. The building blocks were used to effect conjugation to carrier PEG templates which allowed subsequent coupling to a cardiac targeted monoclonal antibody. Immunocompetence of the enediyne-Mab conjugates was demonstrated by ELISA, and both parent enediynes and bioconjugates underwent successful photo-Bergman cyclization. Finally, surface modified (Au) nanoparticle conjugates were prepared and size confirmed by TEM analysis. Application as long-circulating photoactivated prodrugs is anticipated.

Graphical abstractA readily accessible enediyne building block was transformed into a number of conjugates, and photoactivation of the core via the photo-Bergman cyclization effected. Application in the form of immunoconjugates and nanoparticles is demonstrated.Figure optionsDownload full-size imageDownload as PowerPoint slide

Related Topics
Physical Sciences and Engineering Chemistry Organic Chemistry
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