期刊
ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY
卷 8, 期 7, 页码 746-760出版社
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/187152008785914789
关键词
Lamellarins; marine alkaloids; nitrogen heterocycles; cytotoxic agents; topoisomerase I
资金
- CICYT [CTQ2006-03794/BQU]
- Instituto de Salud Carlos III [CB06-01-0074]
- Generalitat de Catalunya [2005SGR 00662]
Lamellarins are a large family of marine alkaloids with potential anticancer activity that have been isolated from diverse marine organisms, mainly ascidians and sponges. All lamellarins feature a 3,4-diarylpyrrole system. Pentacyclic lamellarins, whose polyheterocyclic system has a pyrrole core, are the most active compounds. Some of these alkaloids are potently cytotoxic to various tumor cell lines. To date, Lam-D and Lam-H have been identified as lead compounds for the inhibition of topoisomerase I and HIV-1 integrase, respectively -nuclear enzymes which are over-expressed in deregulation disorders. Moreover, these compounds have been reported for their efficacy in treatment of multi-drug resistant (MDR) tumors cells without mediated drug efflux, as well as their immunomodulatory activity and selectivity towards melanoma cell lines. This article is an overview of recent literature on lamellarins, encompassing their isolation, recent synthetic strategies for their total synthesis, the preparation of their analogs, studies on their mechanisms of action, and their structure-activity relationships (SAR).
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