2. Academic Validation
  3. Synthesis and biological evaluation of 3-amino-, 3-alkoxy- and 3-aryloxy-6-(hetero)arylpyridazines as potent antitumor agents

Synthesis and biological evaluation of 3-amino-, 3-alkoxy- and 3-aryloxy-6-(hetero)arylpyridazines as potent antitumor agents

  • Bioorg Med Chem Lett. 2019 Mar 1;29(5):755-760. doi: 10.1016/j.bmcl.2018.12.050.
Stéphane Sengmany 1,  Mathilde Sitter 1,  Eric Léonel 2,  Erwan Le Gall 1,  Gervaise Loirand 3,  Thierry Martens 1,  Didier Dubreuil 4,  Florian Dilasser 3,  Morgane Rousselle 3,  Vincent Sauzeau 3,  Jacques Lebreton 4,  Muriel Pipelier 4,  Rémy Le Guével 5
Affiliations

Affiliations

  • 1 Electrochimie et Synthèse Organique, Université Paris Est, ICMPE (UMR 7182), CNRS, UPEC, 2 rue Henri Dunant, F-94320 Thiais, France.
  • 2 Electrochimie et Synthèse Organique, Université Paris Est, ICMPE (UMR 7182), CNRS, UPEC, 2 rue Henri Dunant, F-94320 Thiais, France. Electronic address: leonel@icmpe.cnrs.fr.
  • 3 INSERM, UMR1087, CNRS, UNIV Nantes, l'institut du thorax, 8 quai Moncousu - BP 70721, F-44007 Nantes Cedex 1, France.
  • 4 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.
  • 5 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.
PMID: 30655216 DOI: 10.1016/j.bmcl.2018.12.050
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.

Keywords

Arylpyridazines; Biological evaluation; Cytotoxic activity; Electrosynthesis; Nickel catalysis.

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