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新型吡唑甲酰胺衍生物的合成及A549肺癌细胞凋亡或自噬调节剂的发现。

Synthesis of novel pyrazole carboxamide derivatives and discovery of modulators for apoptosis or autophagy in A549 lung cancer cells.

作者信息

Ding Xiao-Ling, Zhang Hai-Yan, Qi Lei, Zhao Bao-Xiang, Lian Song, Lv Hong-Shui, Miao Jun-Ying

机构信息

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

出版信息

Bioorg Med Chem Lett. 2009 Sep 15;19(18):5325-8. doi: 10.1016/j.bmcl.2009.07.131. Epub 2009 Aug 3.

DOI:10.1016/j.bmcl.2009.07.131
PMID:19683442
Abstract

A series of novel 3-aryl-1-arylmethyl-1H-pyrazole-5-carboxamide derivatives 3a-l, were synthesized by the reaction of 3-aryl-1-arylmethyl-1H-pyrazole-5-carbonyl chloride with substituted amine in excellent yields. The compounds 3e-h could suppress A549 lung cancer cell growth. More interestingly, compounds 3e and 3f might inhibit the A549 cell growth by inducing apoptosis; whereas compounds 3g and 3h with fluorine group might inhibit the A549 cell growth by inducing autophagy.

摘要

通过3-芳基-1-芳基甲基-1H-吡唑-5-羰基氯与取代胺反应,以优异产率合成了一系列新型3-芳基-1-芳基甲基-1H-吡唑-5-甲酰胺衍生物3a - l。化合物3e - h可抑制A549肺癌细胞生长。更有趣的是,化合物3e和3f可能通过诱导凋亡来抑制A549细胞生长;而含氟基团的化合物3g和3h可能通过诱导自噬来抑制A549细胞生长。

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