Pla Queral, DanielFrancesch, AndrésCalvo, PilarCuevas, CarmenAligué i Alemany, Rosa MariaAlbericio Palomera, FernandoÁlvarez Domingo, Mercedes2014-07-182014-07-182009-05-271043-1802https://hdl.handle.net/2445/56043Herein is reported the design and synthesis of poly(ethylene glycol) derivatives of Lamellarin D with the aim of modulating their physicochemical properties, and improving the biological activity. Mono-, di- and tri-PEG conjugates with improved solubility were obtained in 18-57% overall yields from the corresponding partially protected phenolic derivatives of Lamellarin D. Conjugates 1-9 were tested in a panel of three human tumor cell lines (MDA-MB-231 breast, A-549 lung and HT-29 colon) to evaluate their cytotoxicity. Several compounds exhibited enhanced cellular internalization, and more than 85% of the derivatives showed a lower GI50 than Lam-D. Furthermore, cell cycle arrest at G2 phase, and apoptotic cell-death pathways were determined for Lamellarin D and these derivatives.12 p.application/pdfeng(c) American Chemical Society , 2009Compostos heterocíclicsMedicaments antineoplàsticsTransport biològicIsoquinolinaHeterocyclic compoundsAntineoplastic agentsBiological transportIsoquinolineinfo:eu-repo/semantics/article5649622014-07-18info:eu-repo/semantics/openAccess19472995