title: Photoactivated enediynes as targeted antitumoral agents: efficient routes to antibody and gold nanoparticle conjugates.
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.
authors.affiliation: Bioorganic and Medicinal Chemistry Laboratories, Department of Chemistry and Chemical Biology, Northeastern University, Boston, MA 02115, USA.
authors.forename: Danielle
authors.initials: D
authors.lastname: Falcone
authors.forename: Jane
authors.initials: J
authors.lastname: Li
authors.forename: Amit
authors.initials: A
authors.lastname: Kale
authors.forename: Graham B
authors.initials: GB
authors.lastname: Jones
mesh_terms: D000911:Antibodies, Monoclonal / Q000737:chemistry* / Q000494:pharmacology*; D003500:Cyclization; D053281:Enediynes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D006046:Gold / Q000737:chemistry*; D015394:Molecular Structure; D053758:Nanoparticles / Q000737:chemistry* / Q000648:ultrastructure; D010777:Photochemistry; D011092:Polyethylene Glycols / Q000737:chemistry*
chemical_list: D000911:Antibodies, Monoclonal; D053281:Enediynes; D011092:Polyethylene Glycols; D006046:Gold