高等学校化学学报2024，Vol.45Issue(4)：90-100,11.DOI:10.7503/cjcu20230520
胡椒碱-双环酰胺衍生物的设计、合成及抗宫颈癌活性
Design,Synthesis and Anti-cervical Cancer Activity of Piperine-bicycloamide Derivatives
摘要
Abstract
In this paper,a series of piperine-dicycloamide derivatives was synthesized using piperine as parent nucleus,and their structures were confirmed by means of nuclear magnetic resonance hydrogen spectroscopy(1H NMR),nuclear magnetic resonance carbon spectroscopy(13C NMR)and high-resolution mass spectrometry(HRMS).Methyl thiazolyl tetrazolium(MTT)assay showed that these compounds had good inhibitory effects on kidney cells(293T),cervical cancer(HeLa)and breast cancer(MD-MB-321).Most derivatives had better inhibitory activity on HeLa cells than positive controls fluorouracil(5-FU)and piperine,and compound 6b had the highest anti-proliferative activity on HeLa cells.The half maximal inhibitory concentration(IC50)of MDA-MB-321 cells was 3.49 μmol/L,and the IC50 of MDA-MB-321 cells was 20.89 μmol/L.The mechanism study showed that compound 6b not only effectively inhibited the migration,invasion,adhesion and cloning ability of HeLa cells,but also showed a strong inhibitory effect on the growth of xenografts of HeLa cells.Therefore,compound 6b has the potential to be a lead compound in tumor therapy.关键词
胡椒碱/抗肿瘤/胡椒碱-双环酰胺衍生物Key words
Piperine/Anti-tumor/Piperine-bicycloamide derivative分类
化学化工引用本文复制引用
王秀军,耿婷,张思懿,刘星,马少杰,刘彬,杨明利,吉敬,姜文韬,何景粱,陈慧杰,乔悦,王德伟,王炳岩,侯啸,刘伟..胡椒碱-双环酰胺衍生物的设计、合成及抗宫颈癌活性[J].高等学校化学学报,2024,45(4):90-100,11.基金项目
江苏海洋大学江苏省海洋药物活性分子筛选重点实验室开放课题(批准号:HY202302,HY202305)、连云港市海产品检验技术研究重点实验室运行费(批准号:5507018036)和江苏省研究生实践创新计划课题(批准号:SY202352X1)资助. Supported by the Open Project of the Key Laboratory of Active Molecular Screening for Marine Drugs in Jiangsu Province,Jiangsu Ocean University,China(Nos.HY202302,HY202305),the Operating Fee of the Key Laboratory of Marine Product Inspection Technology in Lianyungang City,China(No.5507018036),and the Jiangsu Graduate Practice Innovation Program Project,China(No.SY202352X1). （批准号:HY202302,HY202305）
