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新型1-芳基甲基-3-芳基-1H-吡唑-5-碳酰肼衍生物作为抗A549肺癌细胞潜在药物的合成及其构效关系

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

作者信息

Xia Yong, Dong Zhi-Wu, Zhao Bao-Xiang, Ge Xiao, Meng Ning, Shin Dong-Soo, Miao Jun-Ying

机构信息

Institute of Organic Chemistry, School of Chemistry and Chemical Engineering, Shandong University, Jinan 250100, China.

出版信息

Bioorg Med Chem. 2007 Nov 15;15(22):6893-9. doi: 10.1016/j.bmc.2007.08.021. Epub 2007 Aug 21.

Abstract

A series of novel 1-arylmethyl-3-aryl-1H-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 logP values in the range of 3.12-4.94 had more inhibitory effects on the growth of A549 cells.

摘要

合成了一系列新型的1-芳基甲基-3-芳基-1H-吡唑-5-碳酰肼衍生物,并研究了所有化合物对A549细胞生长的影响。结果表明,所有九种化合物均对A549细胞的生长具有抑制作用并诱导细胞凋亡。对化合物的构效关系和脂溶性预测的研究表明,logP值在3.12-4.94范围内的化合物对A549细胞的生长具有更强的抑制作用。

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