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Lamellarin D bioconjugates II: synthesis and cellular internalization of dendrimer and nuclear location signal derivatives
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
Universitat de Barcelona
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.
Compostos heterocíclics
Medicaments antineoplàstics
Productes naturals marins
Transport biològic
Isoquinolina
Heterocyclic compounds
Antineoplastic agents
Marine natural products
Biological transport
Isoquinoline
(c) American Chemical Society , 2009
Artículo
info:eu-repo/semantics/acceptedVersion
American Chemical Society
         

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