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Synthesis and structure - Activity relationship study of potent cytotoxic analogues of the marine alkaloid Lamellarin D
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The marine alkaloid, Lamellarin D (Lam-D), has shown potent cytotoxicity in numerous cancer cell lines, and was recently identified as a potent topoisomerase I inhibitor. A library of open lactone analogs of Lam-D was prepared from a methyl 5,6-dihydropyrrolo[2,1-a]isoquinoline-3- carboxylate scaffold (1) by introducing various aryl groups through sequential and regioselective bromination, followed by Pd(0)-catalyzed Suzuki cross-coupling chemistry. The compounds were obtained in a 24-44% overall yield, and tested in a panel of three human tumor cell lines, MDA-MB- 231 (breast), A-549 (lung), and HT-29 (colon), to evaluate their cytotoxic potential. From these data the SAR study concluded that more than 75% of the open-chain Lam-D analogs tested showed cytotoxicity in a low micromolar GI50 range.
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PLA QUERAL, Daniel, MARCHAL, Antonio, OLSEN, Christian a., FRANCESCH, Andrés, CUEVAS, Carmen, ALBERICIO PALOMERA, Fernando, ÁLVAREZ DOMINGO, Mercedes. Synthesis and structure - Activity relationship study of potent cytotoxic analogues of the marine alkaloid Lamellarin D. _Journal of Medicinal Chemistry_. 2006. Vol. 49, núm. 11, pàgs. 3257-3268. [consulta: 24 de gener de 2026]. ISSN: 0022-2623. [Disponible a: https://hdl.handle.net/2445/56314]