Phosphoramidate protides of five flavones and their antiproliferative activity against HepG2 and L-O2 cell lines
Phosphoramidate protides of five flavones and their antiproliferative activity against HepG2 and L-O2 cell lines
复制标题
DOI：
10.1016/j.ejmech.2016.02.012
复制
发表时间：
2016-04-13
影响因子：
6.7
通讯作者：
Zhao, Wei-jie
中科院分区：
文献类型：
--
作者：
Li, Yue-qing;Yang, Fei;Zhao, Wei-jie
合成了一系列黄酮-7-氨基磷酸酯衍生物，并测试了其对人肝癌细胞系HepG2和人正常肝细胞系L-O2的体外抗增殖活性。掺入氨基酸丙氨酸的化合物8d、16d和17d对HepG2细胞系表现出高抑制活性，IC50值为9.0μmol/L、5.5μmol/L和6.6μmol/L。除化合物8a、9a和16b外，酰基的引入在对人肝癌HepG2细胞的选择性抑制中发挥了关键作用。化合物8d、16d和17d可以显着诱导HepG2细胞的G2/M停滞。特别地，化合物16d可以导致HepG2细胞的早期凋亡。 (C) 2016 Elsevier Masson SAS。版权所有。
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.