Synthesis of New Pyrazole Hybrids as Potential Anticancer Agents with Xanthine Oxidase Inhibitory Activity

Title:Synthesis of New Pyrazole Hybrids as Potential Anticancer Agents with Xanthine Oxidase Inhibitory Activity

Volume: 22 Issue: 12

Author(s): Abdulrhman Alsayari, Yahya I. Asiri, Abdullatif Bin Muhsinah and Mohd. Zaheen Hassan*

Affiliation:

• Department of Pharmaceutical Chemistry, College of Pharmacy, King Khalid University, Abha 61441, Saudi Arabia

Keywords: Pyrazole, one-pot synthesis, anticancer agents, cytotoxic agents, sulforhodamine B assay, xanthine oxidase inhibitory activity.

Abstract:

Aims: The study aims to synthesize hybrid molecules containing pyrazole and aryldiazenyl/arylhydrazono fragments with promising anticancer activity.

Background: The clinical effectiveness of anticancer drugs is limited by their adverse side effects and patient resistance. Therefore, the development of safer classes of drugs through rational drug design is imperative.

Objective: Considering the anticancer potential of the pyrazole moiety, the study was carried out with the objective of synthesizing some hybrid pyrazole derivatives with anticancer potential.

Methods: The anticancer potential of these pyrazolyl analogues were evaluated by sulforhodamine B assay using three cancer cell lines MCF-7, HepG2, and HCT-116.

Results: HCT-116 was the most sensitive cell line against these pyrazolyl analogues. Among these newly synthesised derivatives, 1-(4-((4-bromophenyl)diazenyl)-3,5-dimethyl-1H-pyrazol-1-yl)-2-(naphthalen-2-yloxy)ethan-1-one (5e) emerged as a promising anticancer agent (IC₅₀ 3.6-24.6 μM), having a xanthine oxidase inhibitory effect (IC₅₀ 10.87 μM). To obtain further insights into the binding interactions of these molecules, molecular docking studies were also carried out.

Conclusion: In summary, our findings suggest that these hybrid pyrazolyl derivatives can be considered as potential lead molecules for anticancer agents.

Cite this article as:

Alsayari Abdulrhman, Asiri I. Yahya, Bin Muhsinah Abdullatif and Hassan Zaheen Mohd.*, Synthesis of New Pyrazole Hybrids as Potential Anticancer Agents with Xanthine Oxidase Inhibitory Activity, Anti-Cancer Agents in Medicinal Chemistry 2022; 22 (12) . https://dx.doi.org/10.2174/1871520622666220110162651