Multi-gram synthesis of a porphyrazine platform for cellular translocation, conjugation to Doxorubicin, and cellular uptake

We report the synthesis of the near infrared (NIR) fluorescent porphyrazine (Pz) 285, with pendant hydroxyl groups, as a non-toxic platform for delivery of conjugated chemotherapeutic agents to tumor cells. Conjugation of Pz 285 to Doxorubicin via an acid labile linker and initial biological studies...

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Veröffentlicht in:Tetrahedron letters 2012-10, Vol.53 (41), p.5475-5478
Hauptverfasser: Trivedi, Evan R., Blumenfeld, Carl M., Wielgos, Todd, Pokropinski, Sharon, Dande, Prasad, Hai, Ton T., Barrett, Anthony G.M., Hoffman, Brian M.
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Sprache:eng
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Zusammenfassung:We report the synthesis of the near infrared (NIR) fluorescent porphyrazine (Pz) 285, with pendant hydroxyl groups, as a non-toxic platform for delivery of conjugated chemotherapeutic agents to tumor cells. Conjugation of Pz 285 to Doxorubicin via an acid labile linker and initial biological studies are reported.
ISSN:0040-4039
1873-3581
DOI:10.1016/j.tetlet.2012.07.087