Abstract
Efficient regioselective syntheses of conjugates of folic acid and cytotoxic agents derived from natural epothilones are described. These folate receptor (FR) targeting compounds are water soluble and incorporate a hydrophilic peptide-based spacer unit and a reducible self-immolative disulfide-based linker system between the FR-targeting ligand and the parent drug.
Copyright 2010 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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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology
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Cell Line, Tumor
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Disulfides / chemistry
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Epothilones / chemical synthesis
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Epothilones / chemistry*
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Epothilones / pharmacology
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Folate Receptors, GPI-Anchored / antagonists & inhibitors*
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Folate Receptors, GPI-Anchored / metabolism
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Folic Acid / chemical synthesis
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Folic Acid / chemistry*
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Folic Acid / pharmacology
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Antineoplastic Agents
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Disulfides
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Epothilones
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Folate Receptors, GPI-Anchored
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Folic Acid