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Synthesis and biological evaluation of 3-amino-, 3-alkoxy- and 3-aryloxy-6-(hetero)arylpyridazines as potent antitumor agents. 2019
Stéphane Sengmany, and
Mathilde Sitter, and
Eric Léonel, and
Erwan Le Gall, and
Gervaise Loirand, and
Thierry Martens, and
Didier Dubreuil, and
Florian Dilasser, and
Morgane Rousselle, and
Vincent Sauzeau, and
Jacques Lebreton, and
Muriel Pipelier, and
Rémy Le Guével
Electrochimie et Synthèse Organique, Université Paris Est, ICMPE (UMR 7182), CNRS, UPEC, 2 rue Henri Dunant, F-94320 Thiais, France.
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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