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- Title
2-Imino 2 H-chromene and 2-(phenylimino) 2 H-chromene 3-aryl carboxamide derivatives as novel cytotoxic agents: synthesis, biological assay, and molecular docking study.
- Authors
Edraki, Najmeh; Iraji, Aida; Firuzi, Omidreza; Fattahi, Yousef; Mahdavi, Mohammad; Foroumadi, Alireza; Khoshneviszadeh, Mehdi; Shafiee, Abbas; Miri, Ramin
- Abstract
The inhibition of AKRB has been recognized as a potential therapeutic approach to the treatment of various types of cancers. A novel series of compounds with imino-2 H-chromen and phenylimino-2 H-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)-2 H-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 AKRB catalytic site.
- Subjects
CARBOXAMIDES; BIOLOGICAL assay; MOLECULAR docking; IMINO compounds; ANTINEOPLASTIC agents; CONDENSATION reactions
- Publication
Journal of the Iranian Chemical Society, 2016, Vol 13, Issue 12, p2163
- ISSN
1735-207X
- Publication type
Article
- DOI
10.1007/s13738-016-0934-7