Please use this identifier to cite or link to this item:
http://hdl.handle.net/2445/56314
Full metadata record
DC Field | Value | Language |
---|---|---|
dc.contributor.author | Pla Queral, Daniel | - |
dc.contributor.author | Marchal, Antonio | - |
dc.contributor.author | Olsen, Christian A. | - |
dc.contributor.author | Francesch, Andrés | - |
dc.contributor.author | Cuevas, Carmen | - |
dc.contributor.author | Albericio Palomera, Fernando | - |
dc.contributor.author | Álvarez Domingo, Mercedes | - |
dc.date.accessioned | 2014-07-25T11:06:34Z | - |
dc.date.available | 2014-07-25T11:06:34Z | - |
dc.date.issued | 2006-05-06 | - |
dc.identifier.issn | 0022-2623 | - |
dc.identifier.uri | http://hdl.handle.net/2445/56314 | - |
dc.description.abstract | 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. | - |
dc.format.extent | 12 p. | - |
dc.format.mimetype | application/pdf | - |
dc.language.iso | eng | - |
dc.publisher | American Chemical Society | - |
dc.relation.isformatof | Versió postprint del document publicat a: http://dx.doi.org/10.1021/jm0602458 | - |
dc.relation.ispartof | Journal of Medicinal Chemistry, 2006, vol. 49, num. 11, p. 3257-3268 | - |
dc.relation.uri | http://dx.doi.org/10.1021/jm0602458 | - |
dc.rights | (c) American Chemical Society , 2006 | - |
dc.source | Articles publicats en revistes (Farmacologia, Toxicologia i Química Terapèutica) | - |
dc.subject.classification | Alcaloides | - |
dc.subject.classification | Productes naturals marins | - |
dc.subject.classification | Compostos heterocíclics | - |
dc.subject.classification | Medicaments antineoplàstics | - |
dc.subject.classification | Isoquinolina | - |
dc.subject.other | Alkaloids | - |
dc.subject.other | Marine natural products | - |
dc.subject.other | Heterocyclic compounds | - |
dc.subject.other | Antineoplastic agents | - |
dc.subject.other | Isoquinoline | - |
dc.title | Synthesis and structure - Activity relationship study of potent cytotoxic analogues of the marine alkaloid Lamellarin D | - |
dc.type | info:eu-repo/semantics/article | - |
dc.type | info:eu-repo/semantics/acceptedVersion | - |
dc.identifier.idgrec | 538580 | - |
dc.date.updated | 2014-07-25T11:06:34Z | - |
dc.rights.accessRights | info:eu-repo/semantics/openAccess | - |
Appears in Collections: | Articles publicats en revistes (Farmacologia, Toxicologia i Química Terapèutica) Articles publicats en revistes (Química Inorgànica i Orgànica) |
Files in This Item:
File | Description | Size | Format | |
---|---|---|---|---|
538580.pdf | 301.11 kB | Adobe PDF | View/Open |
Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.