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Synthesis and structure - Activity relationship study of potent cytotoxic analogues of the marine alkaloid Lamellarin D
Pla Queral, Daniel; Marchal, Antonio; Olsen, Christian A.; Francesch, Andrés; Cuevas, Carmen; Albericio Palomera, Fernando; Álvarez Domingo, Mercedes
Universitat de Barcelona
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.
Alcaloides
Productes naturals marins
Compostos heterocíclics
Medicaments antineoplàstics
Isoquinolina
Alkaloids
Marine natural products
Heterocyclic compounds
Antineoplastic agents
Isoquinoline
(c) American Chemical Society , 2006
Artículo
info:eu-repo/semantics/acceptedVersion
American Chemical Society
         

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