Recent Advances in Lamellarin Alkaloids: Isolation, Synthesis and Activity

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)


Volume 17, 14 Issues, 2017


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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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Editor-in-Chief:
Michelle Prudhomme
Institut de Chimie de Clermont-Ferrand
ICCF-CNRS UMR 6296
Université Clermont Auvergne
Clermont-Ferrand
France


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Recent Advances in Lamellarin Alkaloids: Isolation, Synthesis and Activity



Anti-Cancer Agents in Medicinal Chemistry, 8(7): 746-760.

Author(s): D. Pla, F. Albericio and M Alvarez.

Affiliation: Institute for Research in Biomedicine, Barcelona Science Park, University of Barcelona, E-08028, Barcelona, Spain.

Abstract

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).

Keywords:

Lamellarins, marine alkaloids, nitrogen heterocycles, cytotoxic agents, topoisomerase I.



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Article Details

Volume: 8
Issue Number: 7
First Page: 746
Last Page: 760
Page Count: 15
DOI: 10.2174/187152008785914789
Price: $58
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