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...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.展开更多
基金The Natural Science Foundation of Liaoning province(Grant No.20170540730)
文摘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.
