Facile Preparation of an Orthogonally Protected, pH-Sensitive, Bioconjugate Linker for Therapeutic Applications

We describe the facile, three-step synthesis of an orthogonally protected, pH-sensitive linker (8), based on maleic acid, and report its application to the preparation of a pH-sensitive phospholipid (20) for potential use in drug and gene delivery. In addition, we highlight the benefits of our linke...

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Bibliographic Details
Published inOrganic letters Vol. 6; no. 23; pp. 4245 - 4248
Main Authors Fletcher, Steven, Jorgensen, Michael R, Miller, Andrew D
Format Journal Article
LanguageEnglish
Published WASHINGTON American Chemical Society 11.11.2004
Amer Chemical Soc
Subjects
Chemistry
Chemistry, Organic
Hydrogen-Ion Concentration
Maleates - chemistry
Molecular Structure
Phospholipids - chemistry
Physical Sciences
Science & Technology
DRUG
PHOSPHATIDYLETHANOLAMINE
DAUNOMYCIN
ACID
MECHANISM
GENE-TRANSFER
EFFICIENT
ISOMER
ANHYDRIDE
DELIVERY
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Summary:We describe the facile, three-step synthesis of an orthogonally protected, pH-sensitive linker (8), based on maleic acid, and report its application to the preparation of a pH-sensitive phospholipid (20) for potential use in drug and gene delivery. In addition, we highlight the benefits of our linker over the use of the commercially available cis-aconitic anhydride (4).
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
content type line 23
ISSN:1523-7060
1523-7052
DOI:10.1021/ol0483347