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
Anti-Cancer Agents in Medicinal Chemistry
Title: Recent Advances in Lamellarin Alkaloids: Isolation, Synthesis and Activity
Volume: 8 Issue: 7
Author(s): D. Pla, F. Albericio and M. Alvarez
Affiliation:
Keywords: Lamellarins, marine alkaloids, nitrogen heterocycles, cytotoxic agents, topoisomerase I
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).
Export Options
About this article
Cite this article as:
Pla D., Albericio F. and Alvarez M., Recent Advances in Lamellarin Alkaloids: Isolation, Synthesis and Activity, Anti-Cancer Agents in Medicinal Chemistry 2008; 8 (7) . https://dx.doi.org/10.2174/187152008785914789
DOI https://dx.doi.org/10.2174/187152008785914789 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
An Overview of Highly Optically Pure Chloramphenicol Bases: Applications and Modifications
Mini-Reviews in Medicinal Chemistry Drugs Made of RNA: Development and Application of Engineered RNAs for Gene Therapy
Mini-Reviews in Medicinal Chemistry Carbohydrate Microarray Technology for Functional Glycomics
Current Chemical Biology Effects of Drug Transporters on Pharmacological Responses and Safety
Current Drug Metabolism Synthesis and In Vitro Anti-Lung Cancer Activity of Novel 1, 3, 4, 8- Tetrahydropyrrolo [4, 3, 2-de]quinolin-8(1H)-o ne Alkaloid Analogs
Medicinal Chemistry Budesonide and Phenethyl Isothiocyanate Attenuate DNA Damage in Bronchoalveolar Lavage Cells of Mice Exposed to Environmental Cigarette Smoke
Current Cancer Drug Targets Anticancer Drugs Targeting the Apoptotic Pathway
Medicinal Chemistry Reviews - Online (Discontinued) Anthrax Fusion Protein Therapy of Cancer
Current Protein & Peptide Science Bio-Activities and Syntheses Developments of Triptolides
Mini-Reviews in Organic Chemistry Micro-RNA in Disease and Gene Therapy
Current Drug Discovery Technologies Classification of Aurora B Kinase Inhibitors Using Computational Models
Combinatorial Chemistry & High Throughput Screening Interrelationship Between Periapical Lesion and Systemic Metabolic Disorders
Current Pharmaceutical Design Inhaled Biologics: From Preclinical to Product Approval
Current Pharmaceutical Design Myelodysplastic/Myeloproliferative Neoplasms
Current Cancer Therapy Reviews A Review on Advances in Organoborane-Chemistry: Versatile Tool in Asymmetric Synthesis
Current Organic Synthesis Nitric Oxide: Target for Therapeutic Strategies in Alzheimers Disease
Current Pharmaceutical Design Molecule of the Month
Current Topics in Medicinal Chemistry Cancer Fighting SiRNA-RRM2 Loaded Nanorobots
Pharmaceutical Nanotechnology Neuropathic Pain and Lung Delivery of Nanoparticulate Drugs: An Emerging Novel Therapeutic Strategy
CNS & Neurological Disorders - Drug Targets Effects of Tobacco Nicotine-Derived Nitrosamine Ketone (NNK) Exposures on Brain Alcohol Metabolizing Enzyme Activities
Drug Metabolism Letters