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Design, synthesis and antitumor activity evaluation of novel 2,6-dichloro- 3,5-dinitrotoluene derivatives
Alternative TitleDesign, synthesis and antitumor activity evaluation of novel 2,6-dichloro- 3,5-dinitrotoluene derivatives
Jiao Jiayuan1; Hu Hao2; Wei Siyuan1; Wang Wanqiu1; Lin He1; Chai Baoshan1
2018
Source PublicationJournal of Chinese Pharmaceutical Sciences
ISSN1003-1057
Volume27Issue:3Pages:159-169
AbstractA 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.
Other AbstractA 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.
Keyword6-二氯3 5-二硝基甲苯 细胞毒活性 构效关系
Indexed ByCSCD
Language英语
CSCD IDCSCD:6222166
Citation statistics
Document Type期刊论文
Identifierhttp://ir.imr.ac.cn/handle/321006/154680
Collection中国科学院金属研究所
Affiliation1.中国科学院金属研究所
2.沈阳药科大学
Recommended Citation
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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