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

来源：

PHARMACEUTICAL CHEMISTRY JOURNAL | 2020年 / 54卷 / 03期

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

页码：273 / 278

页数：6

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