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Title: Lamellarin D bioconjugates I: synthesis and cellular internalization of PEG-derivatives
Author: Pla Queral, Daniel
Francesch, Andrés
Calvo, Pilar
Cuevas, Carmen
Aligué i Alemany, Rosa Maria
Albericio Palomera, Fernando
Álvarez Domingo, Mercedes
Keywords: Compostos heterocíclics
Medicaments antineoplàstics
Transport biològic
Heterocyclic compounds
Antineoplastic agents
Biological transport
Issue Date: 27-May-2009
Publisher: American Chemical Society
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 GI50 than Lam-D. Furthermore, cell cycle arrest at G2 phase, and apoptotic cell-death pathways were determined for Lamellarin D and these derivatives.
Note: Versió postprint del document publicat a:
It is part of: Bioconjugate Chemistry, 2009, vol. 20, num. 6, p. 1100-1111
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ISSN: 1043-1802
Appears in Collections:Articles publicats en revistes (Biomedicina)
Articles publicats en revistes (Farmacologia, Toxicologia i Química Terapèutica)

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