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2009-05-27

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Si us plau utilitzeu sempre aquest identificador per citar o enllaçar aquest document: https://hdl.handle.net/2445/56043

Lamellarin D bioconjugates I: synthesis and cellular internalization of PEG-derivatives

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Recurs relacionat

http://dx.doi.org/10.1021/bc800503k

Resum

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.

Matèries

Compostos heterocíclics, Medicaments antineoplàstics, Transport biològic, Isoquinolina

Matèries (anglès)

Heterocyclic compounds, Antineoplastic agents, Biological transport, Isoquinoline

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Col·leccions

Articles publicats en revistes (Farmacologia, Toxicologia i Química Terapèutica)
Articles publicats en revistes (Biomedicina)

Citació

PLA QUERAL, Daniel, et al. Lamellarin D bioconjugates I: synthesis and cellular internalization of PEG-derivatives. Bioconjugate Chemistry. 2009. Vol. 20, num. 6, pags. 1100-1111. ISSN 1043-1802. [consulted: 28 of June of 2026]. Available at: https://hdl.handle.net/2445/56043

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