Design, synthesis, and molecular modelling of pyridazinone and phthalazinone derivatives as protein kinases inhibitors

…, AS El-Etrawy, A Ghiaty, ZK Abdel-Samii…

Index: Elagawany, Mohamed; Ibrahim, Mohamed A.; Ali Ahmed, Hany Emary; El-Etrawy, A.Sh.; Ghiaty, Adel; Abdel-Samii, Zakaria K.; El-Feky, Said A.; Bajorath, Juergen Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 7 p. 2007 - 2013

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Citation Number: 10

Abstract

The design and synthesis of pyridazinone and phthalazinone derivatives are described. Newly synthesized compounds were tested on a panel of four kinases in order to evaluate their activity and potential selectivity. In addition, the promising compounds were tested on four cancer cell lines to examine cytotoxic effects. The compounds inhibited DYRK1A and GSK3 with different activity. SAR analysis and docking calculations were carried out to aid ...