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Marhadour S.,University of Nantes | Marchand P.,University of Nantes | Pagniez F.,University of Nantes | Bazin M.-A.,University of Nantes | And 7 more authors.
European Journal of Medicinal Chemistry | Year: 2012

A novel series of 2,3-diarylimidazo[1,2-a]pyridines was synthesized and evaluated for their antileishmanial activities. Four derivatives exhibited good activity against the promastigote and intracellular amastigote stages of Leishmania major, coupled with a low cytotoxicity against the HeLa human cell line. The impact of compound lipophilicity on antiparasitic activities was investigated by Log D comparison. Although LmCK1 could be the parasitic target for three compounds (13, 18, 21), the inhibition of another target is under study to explain the antileishmanial effect of the most promising compounds. © 2012 Elsevier Masson SAS. All rights reserved.


Luu V.T.,Novartis | Goujon J.-Y.,Atlanchim Pharma | Meisterhans C.,RC Tritec AG | Frommherz M.,Novartis | Bauer C.,Novartis
Journal of Labelled Compounds and Radiopharmaceuticals | Year: 2015

The synthesis of a triple tritiated isotopologue of the CRTh2 antagonist NVP-QAW039 (fevipiprant) with a specific activity >3TBq/mmol is described. Key to the high specific activity is the methylation of a bench-stable dimeric disulfide precursor that is in situ reduced to the corresponding thiol monomer and methylated with [3H3]MeONos having per se a high specific activity. The high specific activity of the tritiated active pharmaceutical ingredient obtained by a build-up approach is discussed in the light of the specific activity usually to be expected if hydrogen tritium exchange methods were applied. Copyright © 2015 John Wiley & Sons, Ltd.


Defaux J.,University of Nantes | Antoine M.,University of Nantes | Antoine M.,Atlanchim Pharma | Le Borgne M.,University of Nantes | And 8 more authors.
ChemMedChem | Year: 2014

As part of our research projects to identify new chemical entities of biological interest, we developed a synthetic approach and the biological evaluation of (7-aryl-1,5-naphthyridin-4-yl)ureas as a novel class of Aurora kinase inhibitors for the treatment of malignant diseases based on pathological cell proliferation. 1,5-Naphthyridine derivatives showed excellent inhibitory activities toward Aurora kinases A and B, and the most active compound, 1-cyclopropyl-3-[7-(1-methyl-1H-pyrazol-4-yl)-1,5-naphthyridin-4-yl]urea (49), displayed IC50 values of 13 and 107 nM against Aurora kinases A and B, respectively. In addition, the selectivity toward a panel of seven cancer-related protein kinases was highlighted. In vitro ADME properties were also determined in order to rationalize the difficulties in correlating antiproliferative activity with Aurora kinase inhibition. Finally, the good safety profile of these compounds imparts promising potential for their further development as anticancer agents. Promising Aurora inhibitors: Herein we report a series of (7-aryl-1,5-naphthyridin-4-yl)ureas as a novel class of nanomolar-range Aurora kinase inhibitors. The described derivatives have good cell-penetration parameters and safety profiles, but their efficiency toward signaling pathways are insufficient to induce cell death. We also highlight their selectivity toward a panel of seven cancer-related protein kinases. Copyright © 2014 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.


Luu V.T.,Novartis | Goujon J.-Y.,Atlanchim Pharma | Meisterhans C.,RC Tritec AG Speicherstrasse CH 9053 Teufen Switzerland | Frommherz M.,Novartis | Bauer C.,Novartis
Journal of Labelled Compounds and Radiopharmaceuticals | Year: 2015

The synthesis of a triple tritiated isotopologue of the CRTh2 antagonist NVP-QAW039 (fevipiprant) with a specific activity >3TBq/mmol is described. Key to the high specific activity is the methylation of a bench-stable dimeric disulfide precursor that is in situ reduced to the corresponding thiol monomer and methylated with [3H3]MeONos having per se a high specific activity. The high specific activity of the tritiated active pharmaceutical ingredient obtained by a build-up approach is discussed in the light of the specific activity usually to be expected if hydrogen tritium exchange methods were applied. © 2015 John Wiley & Sons, Ltd.


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