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Design, synthesis, antibacterial and antitumor activities of novel pyrazolo[3,4-b]pyridine-4-one-5-carboxylic acid derivatives
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Yang-jie LI1, Ke LI1, Guo-qiang HU2, *, Wen-long HUANG3
Acta Pharmaceutica Sinica | 2023, 58(10) : 3070 - 3075
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Acta Pharmaceutica Sinica | 2023, 58(10): 3070-3075
Design, synthesis, antibacterial and antitumor activities of novel pyrazolo[3,4-b]pyridine-4-one-5-carboxylic acid derivatives
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Yang-jie LI1, Ke LI1, Guo-qiang HU2, *, Wen-long HUANG3
Affiliations
  • 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
Published: 2023-10-12 doi: 10.16438/j.0513-4870.2023-0157
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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.

pyrazole  /  pyridinone carboxylic acid  /  pyrazolopyridinone carboxylic acid  /  antibacterial activity  /  antitumor activity
Yang-jie LI, Ke LI, Guo-qiang HU, Wen-long HUANG. Design, synthesis, antibacterial and antitumor activities of novel pyrazolo[3,4-b]pyridine-4-one-5-carboxylic acid derivatives[J]. Acta Pharmaceutica Sinica, 2023 , 58 (10) : 3070 -3075 . DOI: 10.16438/j.0513-4870.2023-0157
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Article Info
doi: 10.16438/j.0513-4870.2023-0157
  • Receive Date：2023-02-15
  • Online Date：2025-11-21
  • Published：2023-10-12
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History
  • Received：2023-02-15
  • Revised：2023-03-24
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Affiliations
    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
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表12种不同金属材料的力学参数
科
Family		 属数
Number of
genus		 种数
Number of
species		 占总种数比例
Percentage of
total species (%)		 属
Genus		 种数
Number of
species		 占总种数比例
Percentage of total
species (%)
鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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