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Article

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Accepted version

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2009-05-27

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Please use this identifier to cite or link to this item: https://hdl.handle.net/2445/56025

Lamellarin D bioconjugates II: synthesis and cellular internalization of dendrimer and nuclear location signal derivatives

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http://dx.doi.org/10.1021/bc800504t

Abstract

The design and synthesis of Lamellarin D conjugates with a nuclear localization signal peptide and a poly(ethylene glycol)-based dendrimer are described. Conjugates 1-4 were obtained in 8-84% overall yields from the corresponding protected Lamellarin D. Conjugates 1 and 4 are 1.4 to 3.3-fold more cytotoxic than the parent compound against three human tumor cell lines(MDA-MB-231 breast, A-549 lung, and HT-29 colon). Besides, conjugates 3, 4 showed a decrease in activity potency in BJ skin fibroblasts, a normal cell culture. Cellular internalization was analyzed and nuclear distribution pattern was observed for 4, which contains a nuclear localization signalling sequence.

Subject

Compostos heterocíclics, Medicaments antineoplàstics, Productes naturals marins, Transport biològic, Isoquinolina

Subject (English)

Heterocyclic compounds, Antineoplastic agents, Marine natural products, Biological transport, Isoquinoline

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

Citation

PLA QUERAL, Daniel, et al. Lamellarin D bioconjugates II: synthesis and cellular internalization of dendrimer and nuclear location signal derivatives. Bioconjugate Chemistry. 2009. Vol. 20, num. 6, pags. 1112-1121. ISSN 1043-1802. [consulted: 12 of August of 2026]. Available at: https://hdl.handle.net/2445/56025

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