Design, synthesis and antitumor activity evaluation of novel 2,6-dichloro- 3,5-dinitrotoluene derivatives

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	Design, synthesis and antitumor activity evaluation of novel 2,6-dichloro- 3,5-dinitrotoluene derivatives
其他题名	Design, synthesis and antitumor activity evaluation of novel 2,6-dichloro- 3,5-dinitrotoluene derivatives
	Jiao Jiayuan 1; Hu Hao 2; Wei Siyuan 1; Wang Wanqiu 1; Lin He 1; Chai Baoshan 1
	2018
发表期刊	Journal of Chinese Pharmaceutical Sciences
ISSN	1003-1057
卷号	27 期号:3 页码:159-169
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.
其他摘要	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.
关键词	6-二氯3 5-二硝基甲苯细胞毒活性构效关系
收录类别	CSCD
语种	英语
CSCD记录号	CSCD:6222166
引用统计
文献类型	期刊论文
条目标识符	http://ir.imr.ac.cn/handle/321006/154680
专题	中国科学院金属研究所
作者单位	1.中国科学院金属研究所 2.沈阳药科大学
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.