Synthesis and structure–activity relationships of novel 1-arylmethyl-3-aryl-1 H-pyrazole-5-carbohydrazide derivatives as potential agents against A549 lung cancer cells

1-Arylmethyl-3-aryl-1 H-pyrazole-5-carbohydrazide derivatives were synthesized, and their effects on A549 cell growth and apoptosis were evaluated. The structure–activity relationships and prediction of lipophilicity of compounds were studied. A series of novel 1-arylmethyl-3-aryl-1 H-pyrazole-5-car...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry 2007, Vol.15 (22), p.6893-6899
Main Authors: Xia, Yong, Dong, Zhi-Wu, Zhao, Bao-Xiang, Ge, Xiao, Meng, Ning, Shin, Dong-Soo, Miao, Jun-Ying
Format: Article
Language:English
Subjects:
A549 cells
Antineoplastic agents
Apoptosis
Biological and medical sciences
General aspects
Medical sciences
Pharmacology. Drug treatments
Pyrazole carbohydrazide
Structure–activity relationship
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Summary:1-Arylmethyl-3-aryl-1 H-pyrazole-5-carbohydrazide derivatives were synthesized, and their effects on A549 cell growth and apoptosis were evaluated. The structure–activity relationships and prediction of lipophilicity of compounds were studied. A series of novel 1-arylmethyl-3-aryl-1 H-pyrazole-5-carbohydrazide derivatives were synthesized, and the effects of all the compounds on A549 cell growth were investigated. The results showed that all the nine compounds had inhibitory effects on the growth of A549 cells and induced the cell apoptosis. The study on structure–activity relationships and prediction of lipophilicities of compounds showed that compounds with log P values in the range of 3.12–4.94 had more inhibitory effects on the growth of A549 cells.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2007.08.021