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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 Isoquinolina Heterocyclic compounds Antineoplastic agents Marine natural products Biological transport Isoquinoline |
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: http://dx.doi.org/10.1021/bc800504t |
It is part of: | Bioconjugate Chemistry, 2009, vol. 20, num. 6, p. 1112-1121 |
URI: | http://hdl.handle.net/2445/56025 |
Related resource: | http://dx.doi.org/10.1021/bc800504t |
ISSN: | 1043-1802 |
Appears in Collections: | Articles publicats en revistes (Farmacologia, Toxicologia i Química Terapèutica) |
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