2-Imino 2H-chromene and 2-(phenylimino) 2H-chromene 3-aryl carboxamide derivatives as novel cytotoxic agents: synthesis,biological assay,and molecular docking study |
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| Authors: | Najmeh Edraki Aida Iraji Omidreza Firuzi Yousef Fattahi Mohammad Mahdavi Alireza Foroumadi Mehdi Khoshneviszadeh Abbas Shafiee Ramin Miri |
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| Affiliation: | 1.Medicinal and Natural Products Chemistry Research Center,Shiraz University of Medical Sciences,Shiraz,Iran;2.Department of Medicinal Chemistry, Faculty of Pharmacy, and Pharmaceutical Sciences Research Center,Tehran University of Medical Sciences,Tehran,Iran |
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| 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. |
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