Synthesis, photophysical properties and biological evaluation of ß-alkylaminoporphyrin for photodynamic therapy.
Bioorg Med Chem
; 24(22): 6040-6047, 2016 11 15.
Article
em En
| MEDLINE
| ID: mdl-27713013
ABSTRACT
A series of ß-alkylaminoporphyrins conjugated with different amines at ß position (D1-D3) or with electron-donating and electron-withdrawing substituents at phenyl position (D4-D6) were synthesized. Their photophysical and photochemical properties, intracellular localization, photocytotoxicities in vitro and vivo were also investigated. All target compounds exhibited no cytotoxicities in the dark and excellent photocytotoxicities against HeLa cells. Among them, D6 showed the highest phototoxicity and the lowest dark toxicity, which was more phototoxic than Hematoporphyrin monomethyl ether (HMME). In addition, D6 exhibited best photodynamic antitumor efficacy on BALB/c nude mice bearing HeLa tumor. Therefore, D6 is a powerful and promising antitumor photosensitizer for photodynamic therapy.
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Texto completo:
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Base de dados:
MEDLINE
Assunto principal:
Fotoquimioterapia
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Porfirinas
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Antineoplásicos
Limite:
Animals
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Female
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Humans
Idioma:
En
Revista:
Bioorg Med Chem
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2016
Tipo de documento:
Article
País de afiliação:
China