François Estour | Université de Rouen (original) (raw)
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Papers by François Estour
HAL (Le Centre pour la Communication Scientifique Directe), Oct 6, 2016
National audienc
HAL (Le Centre pour la Communication Scientifique Directe), Oct 6, 2015
International audienc
Heterocycles, 1999
ABSTRACT
HAL (Le Centre pour la Communication Scientifique Directe), Mar 18, 2021
Heterocycles, 2005
Three synthetic approaches to N-substituted Thalidomide prodrugs from (S)-phtaloylglutamic acid, ... more Three synthetic approaches to N-substituted Thalidomide prodrugs from (S)-phtaloylglutamic acid, (S)-Boc-glutamic acid or phtaloylglutamic anhydride are described and compared. The most efficient method is a one-pot synthesis which allowed to obtain an ester derivative of Thalidomide with 67 % yield.
ChemInform, Mar 9, 2004
In order to examine the biotransformations of xenobiotics, it is essential to realize studies of ... more In order to examine the biotransformations of xenobiotics, it is essential to realize studies of metabolism of drugs in living animals. It is generally difficult to extract quantitatively the metabolites from biological media or excreta. Alternative methods have then been developed. Application of such techniques to 4a-methylhexahydronaphthalenones, which constitute starting material for the stereospecific synthesis of terpenoids or steroids, is particularly demonstrative. By biosynthetical ways, it was not possible to access with good yields to all the metabolites obtained in vivo. A novel methodology, based on the use of a manganoporphyrin catalyst, allowed to synthezise large amounts of several models of metabolites corresponding to those which had been isolated in living rats. Only one of the metabolites obtained in vivo could not be synthezised by this biomimetic system. This proved that alternative methods are precious to obtain models with good yields, but need to be validated by controls in living animals.
RSC Advances, 2021
Magnetic resonance imaging (MRI) is a powerful tool for non-invasive, high-resolution three-dimen... more Magnetic resonance imaging (MRI) is a powerful tool for non-invasive, high-resolution three-dimensional medical imaging of anatomical structures such as organs and tissues. The use of contrast agents based on gadolinium chelates started in 1988 to improve the quality of the image, since researchers and industry focused their attention on the development of more efficient and stable structures. This review is about the state of the art of MRI contrast agents based on cyclodextrin scaffolds. Chemical engineering strategies are herein reported including host-guest inclusion complexation and covalent linkages. It also offers descriptions of the MRI properties and in vitro and in vivo biomedical applications of these emerging macrostructures. It highlights that these supramolecular associations can improve the image contrast, the sensitivity, and the efficiency of MRI diagnosis by targeting cancer tumors and other diseases with success proving the great potential of this natural macrocycle.
HAL (Le Centre pour la Communication Scientifique Directe), 2011
HAL (Le Centre pour la Communication Scientifique Directe), May 29, 2017
ChemInform, May 19, 2010
The conditions of the use of the manganese/porphyrin/imidazole system needed to be improved in or... more The conditions of the use of the manganese/porphyrin/imidazole system needed to be improved in order to obtain larger amounts of models of metabolites. An increase of the oxidation yields and a better preservation of this catalytic system have been obtained on the examples of various alkanes, by an acid addition in the reaction mixture. Three manganoporphyrins were checked for evaluation of the reaction. These results were extended to molecules of therapeutical interest such as ibuprofen and phenylbutazone.
Organic and Biomolecular Chemistry, 2017
médecine/sciences
Le Double Cursus Santé Sciences (DCSS) permet de former précocement les futurs acteurs de santé à... more Le Double Cursus Santé Sciences (DCSS) permet de former précocement les futurs acteurs de santé à la recherche. La profonde transformation du système de santé et l’avènement de nouvelles techniques analytiques et numériques ont conduit à reconsidérer la place de la recherche dans la pratique clinique. L’expérience internationale de ce type de programme de formation, notamment aux États-Unis, a révélé le rôle prépondérant que jouent les acteurs de santé ayant acquis une double compétence, médicale et scientifique. En France, un DCSS précoce, pendant les études médicales, a été mis en place dans les années 2000. Cette formation reste cependant disparate et hétérogène, et ne concerne pas toutes les universités. En 2016, l’UFR Santé de Rouen a constaté que le nombre d’étudiants engagés dans ce double cursus était très faible, voire nul selon les années. Aussi, en 2017, un accompagnement institutionnel a été introduit. Celui-ci a abouti à la création d’un tutorat étudiant dédié à cette f...
HAL (Le Centre pour la Communication Scientifique Directe), 2017
HAL (Le Centre pour la Communication Scientifique Directe), Oct 11, 2018
![Research paper thumbnail of Efficient synthesis of imidazopyridodiazepines from peri annulation in imidazo[1,2-a]pyridine](https://attachments.academia-assets.com/112987725/thumbnails/1.jpg)
](Tetrahedron Letters, 2002
Fused pyridine derivatives Fused pyridine derivatives R 0450 Efficient Synthesis of Imidazopyrido... more Fused pyridine derivatives Fused pyridine derivatives R 0450 Efficient Synthesis of Imidazopyridodiazepines from peri Annulation in Imidazo[1,2-a]pyridine.-Condensation of the 3-amino imidazo[1,2-a]pyridine (I) with α,β-unsaturated aldehydes followed by thermal cyclization affords the title compounds (IV) related to non-nucleoside HIV-1 reverse transcriptase inhibitors.-(TEULADE*,
HAL (Le Centre pour la Communication Scientifique Directe), Oct 6, 2016
National audienc
HAL (Le Centre pour la Communication Scientifique Directe), Oct 6, 2015
International audienc
Heterocycles, 1999
ABSTRACT
HAL (Le Centre pour la Communication Scientifique Directe), Mar 18, 2021
Heterocycles, 2005
Three synthetic approaches to N-substituted Thalidomide prodrugs from (S)-phtaloylglutamic acid, ... more Three synthetic approaches to N-substituted Thalidomide prodrugs from (S)-phtaloylglutamic acid, (S)-Boc-glutamic acid or phtaloylglutamic anhydride are described and compared. The most efficient method is a one-pot synthesis which allowed to obtain an ester derivative of Thalidomide with 67 % yield.
ChemInform, Mar 9, 2004
In order to examine the biotransformations of xenobiotics, it is essential to realize studies of ... more In order to examine the biotransformations of xenobiotics, it is essential to realize studies of metabolism of drugs in living animals. It is generally difficult to extract quantitatively the metabolites from biological media or excreta. Alternative methods have then been developed. Application of such techniques to 4a-methylhexahydronaphthalenones, which constitute starting material for the stereospecific synthesis of terpenoids or steroids, is particularly demonstrative. By biosynthetical ways, it was not possible to access with good yields to all the metabolites obtained in vivo. A novel methodology, based on the use of a manganoporphyrin catalyst, allowed to synthezise large amounts of several models of metabolites corresponding to those which had been isolated in living rats. Only one of the metabolites obtained in vivo could not be synthezised by this biomimetic system. This proved that alternative methods are precious to obtain models with good yields, but need to be validated by controls in living animals.
RSC Advances, 2021
Magnetic resonance imaging (MRI) is a powerful tool for non-invasive, high-resolution three-dimen... more Magnetic resonance imaging (MRI) is a powerful tool for non-invasive, high-resolution three-dimensional medical imaging of anatomical structures such as organs and tissues. The use of contrast agents based on gadolinium chelates started in 1988 to improve the quality of the image, since researchers and industry focused their attention on the development of more efficient and stable structures. This review is about the state of the art of MRI contrast agents based on cyclodextrin scaffolds. Chemical engineering strategies are herein reported including host-guest inclusion complexation and covalent linkages. It also offers descriptions of the MRI properties and in vitro and in vivo biomedical applications of these emerging macrostructures. It highlights that these supramolecular associations can improve the image contrast, the sensitivity, and the efficiency of MRI diagnosis by targeting cancer tumors and other diseases with success proving the great potential of this natural macrocycle.
HAL (Le Centre pour la Communication Scientifique Directe), 2011
HAL (Le Centre pour la Communication Scientifique Directe), May 29, 2017
ChemInform, May 19, 2010
The conditions of the use of the manganese/porphyrin/imidazole system needed to be improved in or... more The conditions of the use of the manganese/porphyrin/imidazole system needed to be improved in order to obtain larger amounts of models of metabolites. An increase of the oxidation yields and a better preservation of this catalytic system have been obtained on the examples of various alkanes, by an acid addition in the reaction mixture. Three manganoporphyrins were checked for evaluation of the reaction. These results were extended to molecules of therapeutical interest such as ibuprofen and phenylbutazone.
Organic and Biomolecular Chemistry, 2017
médecine/sciences
Le Double Cursus Santé Sciences (DCSS) permet de former précocement les futurs acteurs de santé à... more Le Double Cursus Santé Sciences (DCSS) permet de former précocement les futurs acteurs de santé à la recherche. La profonde transformation du système de santé et l’avènement de nouvelles techniques analytiques et numériques ont conduit à reconsidérer la place de la recherche dans la pratique clinique. L’expérience internationale de ce type de programme de formation, notamment aux États-Unis, a révélé le rôle prépondérant que jouent les acteurs de santé ayant acquis une double compétence, médicale et scientifique. En France, un DCSS précoce, pendant les études médicales, a été mis en place dans les années 2000. Cette formation reste cependant disparate et hétérogène, et ne concerne pas toutes les universités. En 2016, l’UFR Santé de Rouen a constaté que le nombre d’étudiants engagés dans ce double cursus était très faible, voire nul selon les années. Aussi, en 2017, un accompagnement institutionnel a été introduit. Celui-ci a abouti à la création d’un tutorat étudiant dédié à cette f...
HAL (Le Centre pour la Communication Scientifique Directe), 2017
HAL (Le Centre pour la Communication Scientifique Directe), Oct 11, 2018
Tetrahedron Letters, 2002
Fused pyridine derivatives Fused pyridine derivatives R 0450 Efficient Synthesis of Imidazopyrido... more Fused pyridine derivatives Fused pyridine derivatives R 0450 Efficient Synthesis of Imidazopyridodiazepines from peri Annulation in Imidazo[1,2-a]pyridine.-Condensation of the 3-amino imidazo[1,2-a]pyridine (I) with α,β-unsaturated aldehydes followed by thermal cyclization affords the title compounds (IV) related to non-nucleoside HIV-1 reverse transcriptase inhibitors.-(TEULADE*,