Design, synthesis, antibacterial and antitumor activities of novel pyrazolo3,4-bpyridine-4-one-5-carboxylic acid derivatives
10.16438/j.0513-4870.2023-0157
- VernacularTitle:新型吡唑并[3,4-b]吡啶-4-酮-5-羧酸类化合物的合成及抗菌抗肿瘤活性
- Author:
Yang-jie LI
1
;
Ke LI
1
;
Guo-qiang HU
2
;
Wen-long HUANG
3
Author Information
1. Henan Engineering Technology Research Center of Water Environment and Health, Zhengzhou University of Industrial Technology, Zhengzhou 451150, China
2. School of Clinical Medicine, Henan University, Kaifeng 475004, China
3. Center of Drug Discovery, China Pharmaceutical University, Nanjing 210009, China
- Publication Type:Research Article
- Keywords:
pyrazole;
pyridinone carboxylic acid;
pyrazolopyridinone carboxylic acid;
antibacterial activity;
antitumor activity
- From:
Acta Pharmaceutica Sinica
2023;58(10):3070-3075
- CountryChina
- Language:Chinese
-
Abstract:
To discover new structural hits, based on the important role of pyrazole ring and fragment of pyridinone carboxylic acid in drug design, novel title pyrazolo[3,4-b]pyridine-4-one-5-carboxylic acid derivatives (10a-10p) were designed and synthesized, the structures were confirmed by spectral data and elemental analyses. The antibacterial and antitumor activities were evaluated by the measured minimum inhibitory concentration (MIC) values against the tested four strains and half inhibitory concentration (IC50) values against the tested four cancer cells, respectively. The results displayed markedly poor antibacterial activity and observably potent antitumor activity. In particularly, the title difluorophenyl (10d, 10e, 10f), pyridyl (10j), ethyl (10k) and cycloproyl (10l) compounds exhibited comparable activity against Capan-1 and A549 cells to that of the comparison doxorubicin. Thus, pyrazolo[3,4-b]pyridine-4-one-5-carboxylic acid derivatives as promising antitumor hits need to be developed.
