Pla Queral, DanielMartí, MarcFarrera Sinfreu, Josep MariaPulido, DanielFrancesch, AndrésCalvo, PilarCuevas, CarmenRoyo Expósito, MiriamAligué i Alemany, Rosa MariaAlbericio Palomera, FernandoÁlvarez Domingo, Mercedes2014-07-182014-07-182009-05-271043-1802https://hdl.handle.net/2445/56025The 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.10 p.application/pdfeng(c) American Chemical Society , 2009Compostos heterocíclicsMedicaments antineoplàsticsProductes naturals marinsTransport biològicIsoquinolinaHeterocyclic compoundsAntineoplastic agentsMarine natural productsBiological transportIsoquinolineinfo:eu-repo/semantics/article5649632014-07-18info:eu-repo/semantics/openAccess