Abstract
Oxazole-containing macrolides (1-5) isolated from the marine sponge Chondrosia corticata were evaluated for their actin depolymerizing activities by monitoring fluorescent intensity of pyrene F-actin. These studies led to the identification of (19Z)-halichondramide (5) as a new actin depolymerizing agent. The actin depolymerizing activity by (19Z)-halichondramide (5) was four times more potent than that of halichondramide (1). Compounds 1 and 5 also have potent antifungal activity. The preliminary structure-activity relationship of these compounds is described to elucidate the essential structural requirements.
Copyright © 2011 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antifungal Agents / chemistry
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Antifungal Agents / pharmacology
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Aspergillus fumigatus / drug effects
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Candida albicans / drug effects
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Fluorescence
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Heterocyclic Compounds, 4 or More Rings / chemistry
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Heterocyclic Compounds, 4 or More Rings / pharmacology
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Macrolides / chemistry*
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Macrolides / pharmacology
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Microbial Sensitivity Tests
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Molecular Structure
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Oxazoles / chemistry*
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Oxazoles / pharmacology
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Polymerization / drug effects
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Porifera / chemistry*
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Structure-Activity Relationship
Substances
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(19Z)-halichondramide
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Antifungal Agents
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Heterocyclic Compounds, 4 or More Rings
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Macrolides
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Oxazoles
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halichondramide