Abstract
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 (IC50 4.2 μM), with a potent xanthine oxidase inhibitory activity (IC50 0.83 μM). 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.
Highlights
Cancer is one of the four major types of noncommunicable diseases, along with cardiovascular disease, diabetes, and chronic respiratory diseases [1]. It is a disease in which abnormal cells divide without control and can invade nearby tissues [2]. e cancer burden continues to grow globally, with 18.1 million new cases and 9.6 million deaths in the preceding year [3]
Chemotherapy resistance and its associated serious side effects, even with the targeted therapies, continue to be a major concern for oncologists [5]. erefore, it is imperative that we develop safer and more effective anticancer agents acting through novel mechanisms and target only the cancer cells
Cytotoxicity Assessment. e cytotoxicity of the different compounds was tested against human tumor cells using the sulforhodamine B assay (SRB)
Summary
Pyrazoles are an interesting class of compounds showing potent anticancer activities. Our previous studies have demonstrated the potent anticancer activity of pyrazole analogues. Erefore, we focused on developing anticancer agents through structure optimization of the pyrazolyl lead molecule. E 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. One of the pyrazole derivatives demonstrated the greatest promise as an anticancer agent against the human colon cancer cell line (IC50 4.2 μM), with a potent xanthine oxidase inhibitory activity (IC50 0.83 μM). 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
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a call
