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2-Imino 2H-Chromene and 2-(Phenylimino) 2H-Chromene 3-Aryl Carboxamide Derivatives As Novel Cytotoxic Agents: Synthesis, Biological Assay, and Molecular Docking Study Publisher



Edraki N1 ; Iraji A1 ; Firuzi O1 ; Fattahi Y2 ; Mahdavi M2 ; Foroumadi A2 ; Khoshneviszadeh M1 ; Shafiee A2 ; Miri R1
Authors

Source: Journal of the Iranian Chemical Society Published:2016


Abstract

The inhibition of AKR1B10 has been recognized as a potential therapeutic approach to the treatment of various types of cancers. A novel series of compounds with imino-2H-chromen and phenylimino-2H-chromen scaffolds were synthesized by Knoevenagel condensation reaction. The in vitro cytotoxic activity of synthesized compounds was evaluated against MOLT-4 and SK-OV-3 cells. Among the tested compounds, N-(3,4-dimethoxyphenyl)-2-(phenylimino)-2H-chromene-3-carboxamide (8g) demonstrated potent inhibitory activity against both examined cell lines. The results of the molecular docking study suggested that this compound is involved in critical hydrogen-bonding interactions with the Val301 and Lue302 of AKR1B10 catalytic site. © 2016, Iranian Chemical Society.
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