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

Author(s):

Abdulrhman Alsayari, Yahya I. Asiri, Abdullatif Bin Muhsinah and Mohd. Zaheen Hassan*   Pages 2303 - 2309 ( 7 )

Abstract:

<p>Aims: The study aims to synthesize hybrid molecules containing pyrazole and aryldiazenyl/arylhydrazono fragments with promising anticancer activity. <p> 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. <p> 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. <p> 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. <p> 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. <p> Conclusion: In summary, our findings suggest that these hybrid pyrazolyl derivatives can be considered as potential lead molecules for anticancer agents.</p>

Keywords:

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

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