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Conception et synthese de nouvelles sondes ciblees pour l'imagerie moleculaire

Abstract : Advance in personalized medicine requires probes development for the detection of pathology markers at the earliest possible stage. This thesis describes the synthesis and the evaluation of targeted probes to produce images in MRI or scintigraphy. These probes are constructed by functionalizing a molecular scaffold prepared by a three-component reaction. The resulting propargylamine has the necessary structure to introduce targeting ligands and two chelating agents for imaging. It also has a group in the terminal position to connect it on structures like small polyfunctional molecules, dendrimers or proteins. A high throughput screening technique based on small molecule microarrays was used for the detection of ligands. Molecules spotted on the chip came from either complex C-glycosides prepared according to the concept of diversity-oriented synthesis or from the laboratory chemical library. These microarrays have enable ligand identification for several proteins such as Vpr a protein from the capsid of AIDS virus. A secondary screening by NMR confirmed the interaction between protein and small molecules. Probes carrying a flavonoid for targeting tumor endothelial cells were treated with a gadolinium salt solution and MRI evaluated their properties. Initial results indicated that these compounds does offer of two to four folds contrast than the contrast agents usually used. Their biological evaluation will be conducted soon.
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Contributor : Anne Joubert Connect in order to contact the contributor
Submitted on : Friday, November 25, 2011 - 4:46:38 PM
Last modification on : Wednesday, December 15, 2021 - 10:03:25 AM
Long-term archiving on: : Sunday, February 26, 2012 - 2:35:51 AM


  • HAL Id : pastel-00644998, version 1


Claire Beauvineau. Conception et synthese de nouvelles sondes ciblees pour l'imagerie moleculaire. Chimie thérapeutique. Université Pierre et Marie Curie - Paris VI, 2011. Français. ⟨pastel-00644998⟩



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