Open AccessAnticolon Cancer Properties of Pyrazole Derivatives Acting through Xanthine Oxidase Inhibition
Author(s) -
Abdulrhman Alsayari,
Yahya I. Asiri,
Abdullatif Bin Muhsinah,
Mohd. Zaheen Hassan
Publication year - 2021
Publication title -
journal of oncology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.228
H-Index - 54
eISSN - 1687-8469
pISSN - 1687-8450
DOI - 10.1155/2021/5691982
Subject(s) - pyrazole , xanthine oxidase , sulforhodamine b , combinatorial chemistry , in silico , ic50 , docking (animal) , in vitro , chemistry , biochemistry , pharmacology , stereochemistry , cytotoxicity , medicine , enzyme , nursing , gene
Background Pyrazoles are an interesting class of compounds showing potent anticancer activities. Our previous studies have demonstrated the potent anticancer activity of pyrazole analogues. Therefore, we focused on developing anticancer agents through structure optimization of the pyrazolyl lead molecule.Methods The pyrazole derivatives were prepared by the appropriate synthetic protocols. The antiproliferative activities were evaluated using a sulforhodamine B assay against three cancer cell lines. In vitro and in silico molecular docking studies employing xanthine oxidase were used to explore the mechanism by which pyrazole derivatives exert anticancer effects.Results One of the pyrazole derivatives demonstrated the greatest promise as an anticancer agent against the human colon cancer cell line (IC 50 4.2 μ M), with a potent xanthine oxidase inhibitory activity (IC 50 0.83 μ M).Conclusion In summary, our findings suggest that these pyrazolyl analogues containing a pyridine nucleus could serve as a promising lead molecule in the development of novel anticancer agents.