摘要
经分子杂交技术[A1]合成了一系列4-取代-1-(2-甲基-6-(吡啶-3-基)-烟酰)氨基脲类衍生物.采用噻唑蓝(MTT)比色法研究了目标化合物对人肝癌细胞(QGY-7703)、人肺癌细胞(NCl-H460)和乳腺癌细胞(MCF-7)的体外抗肿瘤活性.1-(2-甲基-6-(吡啶-3-基)烟酰基)-4-(2,4,6-三氯苯基)氨基脲(4n)显示了最优的活性,其半数抑制浓度(IC50)为8.89~11.45 μmol/L.细胞体内的生物研究显示,4n药物[A2]处理能明显增加细胞体内PARP切割水平以及诱导QGY-7703肿瘤细胞的凋亡.
A series of 4-substitued-1-(2-methyl-6-(pyridin-3-yl)-nicotinoyl) semicarbazides were synthesized[A3] via molecular hybridization strategy. The synthesized compounds were screened for their anticancer potential against different cancer cells viz human hepatocelular carcinoma (QGY-7703), non-small cell lung (NCl-H460) and human breast (MCF-7) cancer cell lines by methyl thiazolyl tetrazolium (MTT) assay. 1-(2-Methyl-6-(pyridin-3-yl)nicotinoyl)-4-(2,4,6-trichlorophenyl)semicarbazide (4n) showed significant anticancer activity in these cancer cell lines with a range of IC50 values from 8.89 μmol/L to 11.45 μmol/L. Further biology studies showed that 4n treatment obviously increased the level of cleaved PARP and induced the apoptosis in QGY-7703 cells.
作者
胡鸿雨
吴俊
袁建锋
王珍妮
李晨帆
严晓阳
方美娟
赵胜贤
Hu Hongyu;Wu Jun;Yuan Jianfeng;Wang Zhenni;Li Chenfan;Yan Xiaoyan;Fang Meijuan;Zhao Shengxian(Xingzhi College, Zhejiang Normal University, Jinhua 321004;School of Pharmaceutical Sciences, Xiamen University, Xiamen 361102;College of Science and Technology, Ningbo University, Cixi 315302)
出处
《有机化学》
SCIE
CAS
CSCD
北大核心
2019年第9期2507-2514,共8页
Chinese Journal of Organic Chemistry
基金
Project supported by the General Research Projects of Zhejiang Provincial Department of Education(No.Y201941989)~~
关键词
氨基脲
联吡啶
分子杂交
生物活性
semicarbazides
bipyridine
molecular hybridization
biological activity
