Synthesis and characterization of monophosphinic acid DOTA derivative: A smart tool with functionalities for multimodal imaging
Language English Country Great Britain, England Media print-electronic
Document type Journal Article, Research Support, Non-U.S. Gov't
PubMed
28655418
DOI
10.1016/j.bmc.2017.06.008
PII: S0968-0896(17)30227-4
Knihovny.cz E-resources
- Keywords
- Contrast agents, Gadolinium complex, Macrocyclic ligands, Peptide conjugation, Relaxivity,
- MeSH
- Heterocyclic Compounds, 1-Ring chemical synthesis chemistry MeSH
- Contrast Media chemical synthesis chemistry MeSH
- Magnetic Resonance Imaging MeSH
- Molecular Structure MeSH
- Multimodal Imaging * MeSH
- Mice MeSH
- Dose-Response Relationship, Drug MeSH
- Structure-Activity Relationship MeSH
- Animals MeSH
- Check Tag
- Mice MeSH
- Female MeSH
- Animals MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- 1,4,7,10-tetraazacyclododecane- 1,4,7,10-tetraacetic acid MeSH Browser
- Heterocyclic Compounds, 1-Ring MeSH
- Contrast Media MeSH
A new facile synthetic strategy was developed to prepare bifunctional monophosphinic acid Ln-DOTA derivatives, Gd-DO2AGAPNBn and Gd- DO2AGAPABn. The relaxivities of the Gd-complexes are enhanced compared to Gd-DOTA. Monophosphinic acid arm of these Gd-complexes affords enhancement of inner sphere water exchange rate due to its steric bulkiness. The different functionalities of DO2AGAPNBn were appended in trans positions and are designed to conjugate identical or different vectors according to the potential applications. The conjugation of Gd-DO2AGAPABn with E3 peptide known to target apoptosis was successfully performed and in vivo MRI allowed cell death detection in a mouse model.
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