(E)-4-取代-1-(喹啉-3-基亚甲基)硫代氨基脲的合成及抗肿瘤活性研究  

Synthesis and antitumor activities of N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)hydrazinecarboxamides

作　　者：徐祥斌[1] 胡桑桑 盛含晶 胡鸿雨[2,3] XU Xiang-bin;HU Sang-sang;SHENG Hang-jing;HU Hong-yu(College of Pharmacy and Bioengineering,Hunan Chemical Vocational Technology College,Zhuzhou 412000,China;Xingzhi College,Zhejiang Normal University,Lanxi 321100,China;Key Laboratory of the Ministry of Education for Advanced Catalysis Materials,Zhejiang Normal University,Jinhua 321004,China)

机构地区：[1]湖南化工职业技术学院,制药与生物工程学院,湖南株洲412000 [2]浙江师范大学行知学院,浙江兰溪321100 [3]浙江师范大学“先进催化材料”教育部重点实验室,浙江金华321004

出　　处：《化学研究与应用》2021年第9期1755-1762,共8页Chemical Research and Application

基　　金：金华市科技局公益项目(2019-4-005、2020-4-088)资助;浙江师范大学“先进催化材料”教育部重点实验室和浙江省“固体表面反应化学”重点实验室开放课题基金项目资助。

摘　　要：设计合成(E)-4-取代-1-(喹啉-3-基亚甲基)硫代氨基脲衍生物,并对其体外抗结肠癌性进行研究。以不同硫代异氰酸酯为起始原料,经缩合等反应合成了目标化合物,采用MTT法研究了目标化合物对人结肠癌HCT-116、HCT-8的体外抗肿瘤活性。合成了13个新化合物,其结构经1H-NMR,13C-NMR和HRMS表征。体外生物活性测试结果显示,大多数化合物具有一定的体外抗肿瘤活性,其中化合物3l活性最优,其对HCT-116、HCT-8细胞的半数抑制浓度(IC50)分别为10.10μmol·L^(-1)、9.45μmol·L^(-1)。该系列化合物具有较好的抗肿瘤活性,具有进一步研究的意义。(E)-4-Substituted-1-(quinolin-3-ylmethylene)thiosemicarbazide derivatives were designed and synthesized,and its anti-colon cancer resistance in vitro was studied.Using different thioisocyanates as starting materials,the target compounds were synthesized by condensation and other reactions.The in vitro anti-tumor activities of the target compounds against human colon cancer HCT-116 and HCT-8 were studied by MTT method.Results showed that 13 new compounds were synthesized and their structures were characterized by 1H-NMR,13C-NMR and HRMS.In vitro biological activity test results showed that most compounds had certain in vitro anti-tumor activity,among which compound 3l had the best activity,and its half inhibitory concentration(IC50)on HCT-116 and HCT-8 cells was 10.10μmol·L^(-1) and 9.45,respectively.μmol·L^(-1).This series of compounds had good anti-tumor activity,which was of significance for further research.

关 键 词：氨基脲 喹啉 结肠癌 

分 类 号：O626.4[理学—有机化学]