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

A series of novel 1-arylmethyl-3-aryl-1H-pyrazole-5-carbohydrazide hydrazone derivatives were synthesized and the effects of all the compounds on A549 cell growth were investigated. The results showed that all compounds had almost inhibitory effects on the growth of A549 cells. The study on structur...

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Bibliographic Details
Published in:European journal of medicinal chemistry 2008-11, Vol.43 (11), p.2347-2353
Main Authors: YONG XIA, FAN, Chuan-Dong, ZHAO, Bao-Xiang, JING ZHAO, SHIN, Dong-Soo, MIAO, Jun-Ying
Format: Article
Language:English
Subjects:
Antineoplastic agents
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Biological and medical sciences
Cell Line, Tumor
Cell Survival - drug effects
Crystallography, X-Ray
General aspects
Humans
Inhibitory Concentration 50
Lung Neoplasms - pathology
Medical sciences
Models, Molecular
Molecular Structure
Pharmacology. Drug treatments
Pyrazoles - chemical synthesis
Pyrazoles - chemistry
Pyrazoles - pharmacology
Solubility
Structure-Activity Relationship
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Summary:A series of novel 1-arylmethyl-3-aryl-1H-pyrazole-5-carbohydrazide hydrazone derivatives were synthesized and the effects of all the compounds on A549 cell growth were investigated. The results showed that all compounds had almost inhibitory effects on the growth of A549 cells. The study on structure-activity relationships and prediction of lipophilicities of compounds showed that compounds with LogP values in the range of 4.12-6.80 had inhibitory effects on the growth of A549 cells, and among of them the hydrazone derived from salicylaldehyde had much more inhibitory effects.
ISSN:0223-5234
1768-3254
DOI:10.1016/j.ejmech.2008.01.021