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Brossard D.,Center Detudes Et Of Recherche Sur Le Medicament Of Normandie | Elkihel L.,Center Detudes Et Of Recherche Sur Le Medicament Of Normandie | Khalid M.,Premier University | Rault S.,Center Detudes Et Of Recherche Sur Le Medicament Of Normandie
Synlett | Year: 2010

3-Acetoxy-6-iodocholest-5-ene was prepared with a convenient method from cholesterol and used as a key intermediate for the synthesis of 6-arylated cholesterol derivatives using a Suzuki-Miyaura cross-coupling. This versatile and efficient synthesis way can widely be used in the synthesis of other 6-aryl or 6-heteroaryl steroids as potential drugs. Source


Brossard D.,Center Detudes Et Of Recherche Sur Le Medicament Of Normandie | El Kihel L.,Center Detudes Et Of Recherche Sur Le Medicament Of Normandie | Clement M.,French Institute of Health and Medical Research | Sebbahi W.,Center Detudes Et Of Recherche Sur Le Medicament Of Normandie | And 3 more authors.
European Journal of Medicinal Chemistry | Year: 2010

The novelty of this work derives from the use of nitrogenous heterocycles as building block in the synthesis of conjugate bile acid derivatives. New piperazinyl bile acid derivatives were synthesized and tested in vitro against various human cancer cells (GBM, KMS-11, HCT-116). The best pro-apoptotic activity was obtained with N-[4N-cinnamylpiperazin-1-yl)-3α,7β- dihydroxy-5β-cholan-24-amide (7b) and N-[4N-cinnamyllpiperazin-1-yl)- 3α,7α-dihydroxy-5β-cholan-24-amide (7c) on these human cancer cell lines (IC50: 8.5-31.4 μM). This activity was associated with nuclear and DNA fragmentation, demonstrating that 7b induces cell death by an apoptotic process as 7c. This study shows the possibility of hydrid heterocycle-steroids as new anticancer agents with improved bioactivity and easy to synthesize. © 2010 Elsevier Masson SAS. Source


Gautier B.,University of Paris Descartes | Gautier B.,French Institute of Health and Medical Research | Miteva M.A.,University Paris Diderot | Miteva M.A.,French Institute of Health and Medical Research | And 19 more authors.
Chemistry and Biology | Year: 2011

Protein-protein interactions play a central role in medicine, and their modulation with small organic compounds remains an enormous challenge. Because it has been noted that the macromolecular complexes modulated to date have a relatively pronounced binding cavity at the interface, we decided to perform screening experiments over the vascular endothelial growth factor receptor (VEGFR), a validated target for antiangiogenic treatments with a very flat interface. We focused the study on the VEGFR-1 D2 domain, and 20 active compounds were identified. These small compounds contained a (3-carboxy-2-ureido)thiophen unit and had IC 50 values in the low micromolar range. The most potent compound inhibited the VEGF-induced VEGFR-1 transduction pathways. Our findings suggest that our best hit may be a promising scaffold to probe this macromolecular complex and for the development of treatments of VEGFR-1-dependent diseases. © 2011 Elsevier Ltd. All Rights Reserved. Source


Lozano S.,Center Detudes Et Of Recherche Sur Le Medicament Of Normandie | Poezevara G.,French National Center for Scientific Research | Halm-Lemeille M.-P.,Center Detudes Et Of Recherche Sur Le Medicament Of Normandie | Lescot-Fontaine E.,Center Detudes Et Of Recherche Sur Le Medicament Of Normandie | And 6 more authors.
Journal of Chemical Information and Modeling | Year: 2010

Starting from a random set of structures taken from the European Chemical Bureau (ECB) Web site, an estimation of the classification by acute category in ecotoxicology was carried out. This estimation was based on two approaches. One approach consists in starting with global quantitative structure-ac?ivity relationship (QSAR) equations, analyzing the results and defining an interpretation in terms of overall results and mode of action. The other starts with the notion of emerging fragments and more specifically with the introduction of a particular concept: the jumping fragments. This publication studies the scopes and limitations of each approach for the classification of the derivatives. A promising combination of the two methods is proposed for the classification and also for bringing new information about the importance, for the ecotoxicity, of specific chemical fragments considered alone or in association with others. © 2010 American Chemical Society. Source


Sopkova-de Oliveira Santos J.,Center Detudes Et Of Recherche Sur Le Medicament Of Normandie | Sopkova-de Oliveira Santos J.,University of Paris 13 | Lesnard A.,Center Detudes Et Of Recherche Sur Le Medicament Of Normandie | Agondanou J.-H.,Center Detudes Et Of Recherche Sur Le Medicament Of Normandie | And 9 more authors.
Journal of Chemical Information and Modeling | Year: 2010

In our quest to find new inhibitors able to inhibit acetylcholinesterase (AChE) and, at the same time, to protect neurons from beta amyloid toxicity, i.e., inhibitors interacting with the catalytic anionic subsite as well as with the peripherical anionic site of AChE, a virtual screening of the Centre d'Etudes et de Recherche sur le Médicament de Normandie (CERMN) chemical library was carried out. Two complementary approaches were applied, i.e., a ligand- and a structure-based screening. Each screening led to the selection of different compounds, but only two were present in both screening results. In vitro tests on AChE showed that one of those compounds presented a very good inhibition activity, of the same order as Donepezil. This result shows the real complementary of both methods for the discovery of new ligands. © 2010 American Chemical Society. Source

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