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Title: Lamellarin D bioconjugates II: synthesis and cellular internalization of dendrimer and nuclear location signal derivatives
Author: Pla Queral, Daniel
Martí, M.
Farrera Sinfreu, Josep Maria
Pulido, Daniel
Francesch, Andrés
Calvo, Pilar
Cuevas, Carmen
Royo Expósito, Miriam
Aligué i Alemany, Rosa Maria
Albericio Palomera, Fernando
Álvarez Domingo, Mercedes
Keywords: Compostos heterocíclics
Medicaments antineoplàstics
Productes naturals marins
Transport biològic
Heterocyclic compounds
Antineoplastic agents
Marine natural products
Biological transport
Issue Date: 27-May-2009
Publisher: American Chemical Society
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.
Note: Versió postprint del document publicat a:
It is part of: Bioconjugate Chemistry, 2009, vol. 20, num. 6, p. 1112-1121
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ISSN: 1043-1802
Appears in Collections:Articles publicats en revistes (Farmacologia, Toxicologia i Química Terapèutica)

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