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Lamellarin D bioconjugates I: synthesis and cellular internalization of PEG-derivatives
Pla Queral, Daniel; Francesch, Andrés; Calvo, Pilar; Cuevas, Carmen; Aligué i Alemany, Rosa Maria; Albericio Palomera, Fernando; Álvarez Domingo, Mercedes
Universitat de Barcelona
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 GI50 than Lam-D. Furthermore, cell cycle arrest at G2 phase, and apoptotic cell-death pathways were determined for Lamellarin D and these derivatives.
Compostos heterocíclics
Medicaments antineoplàstics
Transport biològic
Isoquinolina
Heterocyclic compounds
Antineoplastic agents
Biological transport
Isoquinoline
(c) American Chemical Society , 2009
Article
info:eu-repo/semantics/acceptedVersion
American Chemical Society
         

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