Design, synthesis and antitumor activity evaluation of novel 2,6-dichloro- 3,5-dinitrotoluene derivatives | |
Jiao Jiayuan2; Hu Hao1; Wei Siyuan2; Wang Wanqiu2; Lin He2; Chai Baoshan2 | |
刊名 | Journal of Chinese Pharmaceutical Sciences |
2018 | |
卷号 | 27期号:3页码:159-169 |
关键词 | 6-二氯3 5-二硝基甲苯 细胞毒活性 构效关系 |
ISSN号 | 1003-1057 |
其他题名 | Design, synthesis and antitumor activity evaluation of novel 2,6-dichloro- 3,5-dinitrotoluene derivatives |
英文摘要 | A series of novel 2,6-dichloro-3,5-dinitrotoluene derivatives were designed, synthesized in the present study, and their antitumor activities against five cell lines (A431, HepG2, A549, HT -29 and HEK-293) were tested. Most of the compounds exhibited moderate-to-significant cytotoxicity and high selectivity against one or more cell lines in comparison with cisplatin. Studies on their preliminary structure-activity relationships (SARs) indicated that compounds containing phenyl (piperazin-1-yl) methanone groups, especially chlorine atom at 4-position of the phenyl ring, were more effective. Compound 4g was found to be the most potent derivative with IC_(50) values of 1.04, 3.20, 6.93, 4.10 and 20.15 μmol/L against A431, Hep G2, A549, HT-29 and HEK-293 cell lines, respectively, which was better than positive control cisplatin, one of the most clinically used chemotherapeutic drugs. |
语种 | 英语 |
CSCD记录号 | CSCD:6222166 |
内容类型 | 期刊论文 |
源URL | [http://ir.imr.ac.cn/handle/321006/154679] |
专题 | 金属研究所_中国科学院金属研究所 |
作者单位 | 1.沈阳药科大学 2.中国科学院金属研究所 |
推荐引用方式 GB/T 7714 | Jiao Jiayuan,Hu Hao,Wei Siyuan,et al. Design, synthesis and antitumor activity evaluation of novel 2,6-dichloro- 3,5-dinitrotoluene derivatives[J]. Journal of Chinese Pharmaceutical Sciences,2018,27(3):159-169. |
APA | Jiao Jiayuan,Hu Hao,Wei Siyuan,Wang Wanqiu,Lin He,&Chai Baoshan.(2018).Design, synthesis and antitumor activity evaluation of novel 2,6-dichloro- 3,5-dinitrotoluene derivatives.Journal of Chinese Pharmaceutical Sciences,27(3),159-169. |
MLA | Jiao Jiayuan,et al."Design, synthesis and antitumor activity evaluation of novel 2,6-dichloro- 3,5-dinitrotoluene derivatives".Journal of Chinese Pharmaceutical Sciences 27.3(2018):159-169. |
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