Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 20, Issue 15, Pages 4578-4581Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.06.016
Keywords
Folate; Folate receptor targeting; Folate-epothilone conjugate; Disulfide linkers
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Funding
- Endocyte, Inc.
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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. (C) 2010 Elsevier Ltd. All rights reserved.
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