吡唑
化学
组合化学
对接(动物)
黄嘌呤氧化酶
部分
立体化学
小分子
IC50型
体外
药理学
生物化学
生物
酶
医学
护理部
作者
Abdulrhman Alsayari,Yahya I. Asiri,Abdullatif Bin Muhsinah,Mohd. Zaheen Hassan
出处
期刊:Anti-cancer Agents in Medicinal Chemistry
[Bentham Science]
日期:2022-07-01
卷期号:22 (12): 2303-2309
被引量:3
标识
DOI:10.2174/1871520622666220110162651
摘要
Synthesis of hybrid molecules containing pyrazole and aryldiazenyl/arylhydrazono fragments with promising anticancer activity.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 an imperative.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.The anticancer potentials of these pyrazolyl analogues were evaluated by sulforhodamine B assay using three cancer cell lines MCF-7, HepG2 and HCT-116.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.In summary, our findings suggest that these hybrid pyrazolyl derivatives can be considered as potential lead molecules for anticancer agents.
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