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Article Dans Une Revue Journal of Molecular Structure Année : 2019

Synthesis and evaluation of new isatin-aminorhodanine hybrids as PIM1 and CLK1 kinase inhibitors

Résumé

A series of new hybrid isatin-aminorhodanine molecules was prepared by microwave activation under mild conditions. Unexpected condensation of isatin derivatives at C-5 position of aminorhodanine was highlighted and confirmed by NMR and X-ray analyses. The inhibitory activity of these compounds was evaluated towards eight protein kinases, CDK's-2,-5,-9; PIM-1, CLK-1, Haspin, GSK3b and DYRK1A, whose signaling pathway dysregulation is associated to multifactorial diseases such as cancer, inflammatory, cardiovascular, and neurodegenerative diseases. Compound 3l bearing a bromo substituent has shown a potent and selective Pim1 kinase inhibitor activity.
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hal-03870645 , version 1 (24-11-2022)

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Khadidja Khaldoun, Abdelmounaim Safer, Nourdine Boukabcha, Necmi Dege, Sandrine Ruchaud, et al.. Synthesis and evaluation of new isatin-aminorhodanine hybrids as PIM1 and CLK1 kinase inhibitors. Journal of Molecular Structure, 2019, 1192, pp.82 - 90. ⟨10.1016/j.molstruc.2019.04.122⟩. ⟨hal-03870645⟩
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