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

作     者：Jiayuan Jiao Hao Hu Siyuan Wei Wanqiu Wang He Lin Baoshan Chai 焦佳媛;胡浩;魏思源;王婉秋;林鹤;柴宝山

作者机构：Pharmaceutical Research Laboratory Shenyang Research Institute of Chemical lndustry Co. Ltd. Shenyang 110021 China Shenyang Pharmaceutical University Shenyang 110016 China Safety Evaluation Center Shenyang Research Institute of Chemical lndustry Co. Ltd Shenyang 110021 China 

基　　金：The Natural Science Foundation of Liaoning province(Grant No.20170540730) 

出 版 物：《Journal of Chinese Pharmaceutical Sciences》 (中国药学（英文版）)

年 卷 期：2018年第27卷第3期

页      码：159-169页

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, HepG2, A549, HT-29 and HEK-293 cell lines, respectively, which was better than positive control cisplatin, one of the most clinically used chemotherapeutic drugs.

主 题 词：2,6-Dichloro-3,5-dinitrotoluene Cytotoxic activity Structure-activity relationships 

学科分类：1007[医学-药学类] 10[医学] 

核心收录：

D　O　I：10.5246/jcps.2018.03.017

馆 藏 号：203285074...