Synthesis and characterization of monophosphinic acid DOTA derivative: A smart tool with functionalities for multimodal imaging

Satya Narayana Murthy Chilla; Ondrej Zemek; Jan KotekSébastien BoutryLionel LarbanoixCoralie SclavonsLuce Vander ElstIvan LukesRobert N. MullerSophie Laurent

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Synthesis and characterization of monophosphinic acid DOTA derivative: A smart tool with functionalities for multimodal imaging

机译：Synthesis and characterization of monophosphinic acid DOTA derivative: A smart tool with functionalities for multimodal imaging

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Graphical abstract Display Omitted Abstract A new facile synthetic strategy was developed to prepare bifunctional monophosphinic acid Ln-DOTA derivatives, Gd-DO2AGAP NBn and Gd- DO2AGAP ABn . 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 DO2AGAP NBn were appended in trans positions and are designed to conjugate identical or different vectors according to the potential applications. The conjugation of Gd-DO2AGAP ABn 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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来源
《Bioorganic and medicinal chemistry》 |2017年第16期|4297-4303|共7页
作者
Satya Narayana Murthy Chilla; Ondrej Zemek; Jan KotekSébastien BoutryLionel LarbanoixCoralie SclavonsLuce Vander ElstIvan LukesRobert N. MullerSophie Laurent;
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Department of Inorganic Chemistry, Universita Karlova;

Department of General, Organic and Biomedical Chemistry, NMR and Molecular Imaging Laboratory;

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正文语种英语
中图分类药学;
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Contrast agents; Macrocyclic ligands; Peptide conjugation; Gadolinium complex; Relaxivity;

Synthesis and characterization of monophosphinic acid DOTA derivative: A smart tool with functionalities for multimodal imaging

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