Title:
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Lamellarin D bioconjugates II: synthesis and cellular internalization of dendrimer and nuclear location signal derivatives
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Author:
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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
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Other authors:
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Universitat de Barcelona |
Abstract:
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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(s):
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-Compostos heterocíclics -Medicaments antineoplàstics -Productes naturals marins -Transport biològic -Isoquinolina -Heterocyclic compounds -Antineoplastic agents -Marine natural products -Biological transport -Isoquinoline |
Rights:
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(c) American Chemical Society , 2009
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Document type:
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Article Article - Accepted version |
Published by:
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American Chemical Society
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