Design and Synthesis of Novel Pyrazolo[3,4-d]Pyrimidines:In VitroCytotoxic Evaluation and Free Radical Scavenging Activity Studies

被引:9
|
作者
Alharthy, Rima D. [1 ]
机构
[1] King Abdulaziz Univ, Sci & Arts Coll, Dept Chem, Rabigh Campus, Jeddah, Saudi Arabia
关键词
pyrazolo[3; 4-d]pyrimidines; pharmacophore; cytotoxicity; anticancer; radical scavenging activity; BIOLOGICAL EVALUATION; PYRIMIDINE-DERIVATIVES; ANTICANCER; INHIBITORS; PYRAZOLOPYRIMIDINES; KINASE; POTENT;
D O I
10.1007/s11094-020-02190-2
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
With evident biological importance, a new series of pyrazolo[3,4-d]pyrimidines3a,3band4a,4bwere synthesized via the formation of pyrazol-3-one2aand2bsubstrates. All compounds were evaluated forin vitrocytotoxic activity against MCF-7 (breast adenocarcinoma) and A549 (lung cancer) cell lines. The obtained results showed that pyrazolo[3,4-d] pyrimidin-4-ol3abearing phenyl group atN-1 andp-C(6)H(4)atC-6, and4bwith dinitrophenyl atN-1 and furanyl moiety atC-6 had better inhibitory activity against MCF-7 with IC(50)values in a micromolar range as compared to other substrates. The synthesized compounds can be considered as new candidates for further optimization as anticancer agents.
引用
收藏
页码:273 / 278
页数:6
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