4-[二(4-氟苯基)甲基]哌嗪-1-二硫代甲酸酯衍生物的合成及抗肿瘤活性研究
收稿日期: 2016-04-18
修回日期: 2016-07-19
网络出版日期: 2016-08-22
基金资助
四川省科技厅科技支撑计划（No. 2015NZ0033）和西南民族大学大学生创新创业训练基金（No. S201510656121）资助项目.
Synthesis and Antitumor Activities of Alkyl 4-(Bis(4-fluorophenyl)-methyl)piperazine-1-carbodithioate Derivatives
Received date: 2016-04-18
Revised date: 2016-07-19
Online published: 2016-08-22
Supported by
Project supported by the Sichuan Provincial Department of Science and Technology (No. 2015NZ0033) and the Southwest University for Nationalities Students Innovation and Entrepreneurship Training (No. S201510656121).
以1-[二（4-氟苯）甲基]哌嗪、溴代物及二硫化碳为原料，在K3PO4催化下，经一步反应合成了13个新的4-[二（4-氟苯）甲基]哌嗪-1-二硫代甲酸酯衍生物，其结构均经红外、高分辨率质谱、核磁共振氢谱所确证.并进行了体外抗肿瘤活性测试和抑菌活性测试.结果表明，有12个化合物对CDC25B具有抑制作用，其抑制率最高可达99%；有3个化合物对白血病HL-60肿瘤细胞具有抑制作用，其抑制率最高可达54.59%.
关键词： 1-[二(4-氟苯)甲基]哌嗪; 二硫代甲酸酯; 有机合成; 抗肿瘤活性
邓杰 , 李爱暖 , 李清寒 , 丁勇 , 杨学军 , 陈峰 . 4-[二(4-氟苯基)甲基]哌嗪-1-二硫代甲酸酯衍生物的合成及抗肿瘤活性研究[J]. 有机化学, 2016 , 36(12) : 2981 -2985 . DOI: 10.6023/cjoc201604037
Thirteen new alkyl 4-(bis(4-fluorophenyl)methyl)piperazine-1-carbodithioatee derivatives were synthesized with 1-(bis(4-fluorophenyl)methyl)piperazine, substituted benzyl or alkyl bromide and methane-dithione as starting material in the presence of K3PO4. Their structures were determined by IR, MS and 1H NMR. Preliminary bioassay indicated that twelve compounds exhibited good activities against CDC25B (the inhibition rates up to 99% at the concentration of 20 μg/mL), three compounds exhibited a certain degree against Leukemia HL-60 cell (the inhibition rates up to 54.59% at the concentration of 40 μmol/L).
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