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Updated: Jun 1, 2026

Microwave-Assisted Preparation of 1-Aryl-1H-pyrazole-5-amines
Published on: June 23, 2019
[Synthesis and antitumor activities of pyrimidines]
Wen-wei You1, Pei-liang Zhao, Min Zou
1College of Pharmaceutical Sciences, Southern Medical University, Guangzhou 510515, China. youww@fimmu.com
Objective:
To synthesize cyclin-dependent kinase (CDKs) inhibitors and assay their antitumor activities.
Methods:
A series of pyrimidines containing different arylamino and 1-(methylsulfonyl)piperidin moieties were designed by combining the segments 1-(methylsulfonyl)piperidin and pyrimidine heterocycles according to the super-position principle of the reinforcement of biological activities.
Results:
Their structures were characterized by MS and 1H NMR spectra and all the synthesized compounds were screened for their antimicrobial activity with MTT assay.
Conclusion:
The preliminary bioassay showed that compound 3 b displayed good antitumor activity (IC(50)=13.6 µmol/L). The preliminary structure activity relationship analysis of these analogues suggest that the steric factor may have important impact on the anti-tumor activity.
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