Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 18, Issue 3, Pages 934-937Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2007.12.045
Keywords
enediyne; photo-Bergman; bioconjugation; antibody conjugate; nanoparticles
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Funding
- NIGMS NIH HHS [R01GM57123] Funding Source: Medline
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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 (An) nanoparticle conjugates were prepared and size confirmed by TEM analysis. Application as long-circulating photoactivated prodrugs is anticipated. (C) 2007 Elsevier Ltd. All rights reserved.
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