新型DTC金属配合物的抗肿瘤活性及构像研究

新型DTC金属配合物的抗肿瘤活性及构像研究

贺飞, 黄卉, 尹富玲, 李润涛, 雷小平, 曾慧慧^*

1.北京大学药学院化学生物系, 北京 100083;
2.北京大学药学院药物化学系, 北京 100083

收稿日期:2005-08-12 修回日期:2005-11-10 出版日期:2005-12-15 发布日期:2005-12-15
通讯作者: 曾慧慧*

Conformation and Antitumor Activity of Novel Metal Complexes of Piperazinedithioformates

HE Fei, HUANG Hui, YIN Fu-ling, LI Run-tao, LEI Xiao-ping, ZENG Hui-hui ^*

1. Department of Chemical Biology,School of Pharmaceutical Sciences, Peking University, Beijing 100083, China
2.Department of Medicinal Chemistry,School of Pharmaceutical Sciences, Peking University, Beijing 100083, China

Received:2005-08-12 Revised:2005-11-10 Online:2005-12-15 Published:2005-12-15
Contact: ZENG Hui-hui *

摘要/Abstract

摘要： DTC是一类具有广泛生物活性的化合物。Piperazinedithioformates具有一定的抗肿瘤活性, 但其溶解性却较差。本文对一系列新型的DTC金属配合物就人体六种癌细胞系进行了体外抗肿瘤作用研究, 发现了两个有较好抗肿瘤活性的化合物; 并对SRCu进行构像研究, 第一次得到了其稳定构像。

关键词: DTC, DTC, DTC, 抗肿瘤药物, 抗肿瘤药物, 抗肿瘤药物, 铜, 铜, 铜

Abstract:

The in vitro antitumour efficacy of some novel metal complexes of piperazinedithioformates (SR-M) was examined in six cancer cell lines. The activity was compared with that of piperazinedithioformates. Biological evaluations of a series of SR-M compounds suggest that the compounds 1c (SR-Cu) and 1f (SR-Sn) show a potent antitumor activity. The stable conformation structure of SR-Cu as a representative of SR-M was investigated and confirmed by computer workshop.

Key words: Dithiocarbamates DTC, Dithiocarbamates DTC, antitumor drugs, antitumor drugs, Cu, Cu

中图分类号:

R916.696

R965

Supporting: Foundation item: National Natural Science Foundation of China (20172006).
^*Corresponding author. Tel.: 86-010-82802878

贺飞, 黄卉, 尹富玲, 李润涛, 雷小平, 曾慧慧^*. 新型DTC金属配合物的抗肿瘤活性及构像研究[J]. .

HE Fei, HUANG Hui, YIN Fu-ling, LI Run-tao, LEI Xiao-ping, ZENG Hui-hui ^*. Conformation and Antitumor Activity of Novel Metal Complexes of Piperazinedithioformates[J]. .

[1]	朱刚直, 易勤, 范志宏, 马岳慧, 王丹丹, 王磊, 程泽能. LC-MS/MS法测定大鼠血浆中PAC-1的新型抗癌衍生物的浓度及其药物动力学研究[J]. 中国药学(英文版), 2017, 26(11): 811-818.
[2]	刘忆霜, 王颖, 郑佳音, 李兴华, 关艳, 黄树超, 肖春玲. KL-0153, 一种新型铜绿假单胞菌MexAB-OprM外排泵抑制剂[J]. 中国药学(英文版), 2016, 25(4): 310-315.
[3]	薛清丹, 鞠爱霞, 康宇红, 郑春雨, 李秋红. 甲基莲心碱对阿霉素药动学影响[J]. 中国药学(英文版), 2015, 24(4): 225-230.
[4]	谢英, 王菲, 李菲菲, 李明升, 邓丽丽^* . 苏氨酸双铜配合物对糖尿病小鼠血糖、血脂的影响及对心肾血管的保护作用[J]. , 2007, 16(1): 14-17.
[5]	刘艳, 贾彩, 侯新朴. 脂质体的电性对水杨酸铜SOD样活性的影响[J]. , 2001, 10(2): 94-96.
[6]	徐尚志, 刘耕陶. 银杏叶提取物体外对铜离子诱导的人血清低密度脂蛋白氧化修饰的抑制作用[J]. , 1999, 8(3): 158-162.
[7]	刘艳^*, 张学东, 马思谦, 鲁纯素. Tween 胶束体系中水杨酸铜络合物的SOD样活性[J]. , 1997, 6(1): 23-27.
[8]	应宇辉, 张颖, 鲁纯素. 胶束体系中的水杨酸铜络合物对培养的巨噬细胞释放的超氧离子的清除作用[J]. , 1995, 4(1): 32-36.