Synthesis and biological evaluation of 3-amino-, 3-alkoxy- and 3-aryloxy-6-(hetero)arylpyridazines as potent antitumor agents |
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| Authors: | Stéphane Sengmany Mathilde Sitter Eric Léonel Erwan Le Gall Gervaise Loirand Thierry Martens Didier Dubreuil Florian Dilasser Morgane Rousselle Vincent Sauzeau Jacques Lebreton Muriel Pipelier Rémy Le Guével |
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| Institution: | 1. Electrochimie et Synthèse Organique, Université Paris Est, ICMPE (UMR 7182), CNRS, UPEC, 2 rue Henri Dunant, F-94320 Thiais, France;2. Laboratoire de Synthèse Organique, Chimie et Interdisciplinarité: Synthèse, Analyse, Modélisation, UMR 6513, CNRS-Université de Nantes, 2 rue de la Houssinière, BP 92208, F-44322 Nantes Cedex 3, France;3. INSERM, UMR1087, CNRS, UNIV Nantes, l’institut du thorax, 8 quai Moncousu – BP 70721, F-44007 Nantes Cedex 1, France;4. Plate-Forme ImPACcell, Structure Fédérative de Recherche BIOSIT, Université de Rennes 1, Campus de Villejean, 2 Avenue du Pr. Leon Bernard CS34317, F-35043 Rennes Cedex, France |
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| Abstract: | Various 3-amino-, 3-aryloxy- and alkoxy-6-arylpyridazines have been synthesized by an electrochemical reductive cross-coupling between 3-amino-, 3-aryloxy- or 3-alkoxy-6-chloropyridazines and aryl or heteroaryl halides. In vitro antiproliferative activity of these products was evaluated against a representative panel of cancer cell lines (HuH7, CaCo-2, MDA-MB-231, HCT116, PC3, NCI-H727, HaCaT) and oncogenicity prevention of the more efficient derivatives was highlighted on human breast cancer cell line MDA-MB 468-Luc prior establishing their interaction with p44/42 and Akt-dependent signaling pathways. |
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| Keywords: | Electrosynthesis Nickel catalysis Arylpyridazines Biological evaluation Cytotoxic activity |
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