Synthesis and Cytotoxicity Studies of Novel 2-Hydrazonylpyrido[2,3-b]pyrazin-3(4H)-ones

被引:6
作者
Zhang, Guogang [1 ]
Liu, Yajing [1 ]
Wang, Shuobing [1 ]
Zhou, Chuan [1 ]
Huang, Qingchang [1 ]
Gong, Ping [1 ]
机构
[1] Shenyang Pharmaceut Univ, Key Lab Original New Drugs Design & Discovery, Minist Educ, Sch Pharmaceut Engn, Shenyang 110016, Liaoning, Peoples R China
关键词
Anticancer activity; Apoptosis; 2-Hydrazonylpyrido[2; 3-b]pyrazin-3(4H)-ones; APOPTOSIS; CALPAIN;
D O I
10.1002/ardp.201100103
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
In an attempt to develop potent antitumor agents, a series of novel 2-hydrazonylpyrido[2,3-b]pyrazin-3(4H)-one derivatives were designed and synthesized. All the prepared compounds were screened for their cytotoxic activities against A549, MDA-MB-231 and HT-29 cell lines in vitro. Pharmacological data indicated that five of the target compounds showed cytotoxicity against A549 cell line below a concentration of 1 mu M. Compound 15g was the most potent one with IC50 values of 0.19, 2.11 and 2.15 mu M against A549, MDA-MB-231 and HT29 cell lines, respectively.
引用
收藏
页码:49 / 56
页数:8
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