Lamellarin D bioconjugates I: Synthesis and cellular internalization of PEG-derivatives.
Bioconjug Chem
; 20(6): 1100-11, 2009 Jun.
Article
em En
| MEDLINE
| ID: mdl-19472995
ABSTRACT
Herein is reported the design and synthesis of poly(ethylene glycol) derivatives of Lamellarin D with the aim of modulating their physicochemical properties and improving the biological activity. Mono-, di-, and tri-PEG conjugates with improved solubility were obtained in 18-57% overall yields from the corresponding partially protected phenolic derivatives of Lamellarin D. Conjugates 1-9 were tested in a panel of three human tumor cell lines (MDA-MB-231 breast, A-549 lung, and HT-29 colon) to evaluate their cytotoxicity. Several compounds exhibited enhanced cellular internalization, and more than 85% of the derivatives showed a lower GI(50) than Lam-D. Furthermore, cell cycle arrest at G2 phase and apoptotic cell-death pathways were determined for Lamellarin D and these derivatives.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Polietilenoglicóis
/
Cumarínicos
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Compostos Heterocíclicos de 4 ou mais Anéis
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Isoquinolinas
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Antineoplásicos
Limite:
Humans
Idioma:
En
Ano de publicação:
2009
Tipo de documento:
Article