|
个人信息Personal Information
教授
博士生导师
硕士生导师
性别：男
毕业院校：日本富山医科药科大学
学位：博士
所在单位：化工学院
学科：药物化学. 药物分析学
办公地点：西部新校区G-302室（制药科学与技术学院）
联系方式：84986195
电子邮箱：zyzhao@dlut.edu.cn
Phosphoramidate protides of five flavones and their antiproliferative activity against HepG2 and L-O2 cell lines
点击次数：
论文类型：期刊论文
发表时间：2016-04-13
发表刊物：EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
收录刊物：SCIE、PubMed、Scopus
卷号：112
页面范围：196-208
ISSN号：0223-5234
关键字：Flavone; Phosphoramidate; HepG2; G2/M arrest; Apoptosis
摘要：A series of flavone-7-phosphoramidate derivatives were synthesized and tested for their antiproliferative activity in vitro against human hepatoma cell line HepG2 and human normal hepatic cell line L-O2. Compound 8d, 16d and 17d, incorporating the amino acid alanine, exhibited high inhibitory activity on HepG2 cell line with IC50 values of 9.0 mu mol/L, 5.5 mu mol/L and 6.6 mu mol/L. The introduction of acyl groups played a pivotal role in the selective inhibition toward human hepatoma HepG2 cells, except for compound 8a, 9a and 16b. Compound 8d, 16d and 17d could significantly induce G2/M arrest in HepG2 cells. Specially, Compound 16d could lead early apoptosis in HepG2 cells. (C) 2016 Elsevier Masson SAS. All rights reserved.