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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
biochemistry, genetics and molecular biology
Synthesis and structure-activity relationship study of potent cytotoxic analogues of the marine alkaloid lamellarin D
Journal of Medicinal Chemistry, Volume 49, No. 11, Year 2006
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Description
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 analogues of Lam-D was prepared from a methyl 5,6-dihydropyrrolo[2,1-α]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 analogues tested showed cytotoxicity in a low micromolar GI 50 range. © 2006 American Chemical Society.
Authors & Co-Authors
Francesch, Andrés M.
Spain, Colmenar Viejo
Pharmamar S.a.
Cuevas, Carmen Del Maria
Spain, Colmenar Viejo
Pharmamar S.a.
Alberício, Fernando
Spain, Barcelona
Irb Barcelona - Institute for Research in Biomedicine
Álvarez, Mercedes
Spain, Barcelona
Irb Barcelona - Institute for Research in Biomedicine
Statistics
Citations: 104
Authors: 4
Affiliations: 4
Identifiers
Doi:
10.1021/jm0602458
ISSN:
00222623
Research Areas
Cancer