摘要
根据药效基团拼合原理,苯三甲氧基在黄酮B环上进行结构修饰,再与苯并咪唑类化合物衍生化得到9个全新的3'4'5-三甲氧基-7-羟基黄酮苯并咪唑衍生物。采用MTT法检测化合物的体外抗肿瘤活性。化合物4-12对MGC-803细胞株和MCF-7细胞株更为敏感。其中,化合物8的体外抗肿瘤活性最好,对胃癌细胞MGC-803、乳腺癌细胞MCF-7和肝癌细胞HepG-2的IC_(50)值分别为20.47±2.07μmol/L、43.42±3.56μmol/L和35.45±2.03μmol/L,均优于阳性对照药5-氟尿嘧啶。化合物8具有较强的抗肿瘤活性,值得进一步探究其抗肿瘤活性与活性机制。
In this study,the trimethoxy group was introduced into the B-ring of flavonoid and link benzimidazole and its derivatives to 7-OH with different chain alkanes. The anti-tumor activity of flavonoid benzimidazole derivatives 4-12 was studied by MTT colorimetric assay. On the whole,compounds 4-12 showed better anti-tumor activity against MGC-803 cells and MCF-7 cells. What＇s more,Compound 8 exhibited the most potent anti-proliferative activity against MGC-803 cells,MCF-7 cells and HepG2 cells and the IC_（50） was 20.47± 2.07 μmol/L、43.42± 3.56 μmol/L and 35.45± 2.03 μmol/L,respectively. Compound 8 could be a novel anti-tumor leading compound to further evaluation and investigation.
作者
俞晨泽
袁昊
黄晓敏
郑瑰琼
邓湘萍
王哲
曹轩
唐国涛
YU Chenze;YUAN Hao;HUANG Xiaomin;ZHENG Guiqiong;DENG Xiangping;WANG Zhe;CAO Xuan;TANG Guotao(Institute of Pharmacy and Pharmacology,Hunan Province Cooperative Innovation Center for Molecular Target New Drug Study,University of South China,Hengyang 421001,Hunan,China)
出处
《中南医学科学杂志》
CAS
2018年第4期368-372,391,共6页
Medical Science Journal of Central South China
基金
湖南省大学生研究性学习和创新性实验计划项目(编号0223-0002-00007)
