膦酸酯糖苷衍生物的合成与抗肿瘤活性
DOI:
作者:
作者单位:

作者简介:

通讯作者:

中图分类号:

基金项目:

贵州省科技厅国际合作基金(G[2014]7013)


Synthesis and Antitumor Activity of Glycoside Drivatives Containing Posphonate
Author:
Affiliation:

Fund Project:

Project supported by the Technology Department of Guizhou Province (No. G[2014]7013)

  • 摘要
  • |
  • 图/表
  • |
  • 访问统计
  • |
  • 参考文献
  • |
  • 相似文献
  • |
  • 引证文献
  • |
  • 资源附件
  • |
  • 文章评论
    摘要:

    以α-羟基膦酸酯和溴代单糖为中间体,碱性离子液体[Bmim]OH为催化剂,微波辅助,以79.6%-84.1%的收率合成了系列膦酸酯糖苷化合物(Ⅲa-Ⅲf),经IR, 1HNMR, 13CNMR确认了产物结构。采用溴化噻唑蓝四氮唑 (MTT) 法进行了体外抗肿瘤活性测试。结果表明:该类化合物对人胃癌细胞 (SGC-7901)和人肺癌细胞 (A-549)有增殖抑制作用,其中,含葡萄糖基片段的目标物Ⅲa、Ⅲb对SGC-7901有较优的增殖抑制作用,IC50分别为12.9±0.9μmol/L、14.3±1.1μmol/L;含半乳糖基片段的目标物Ⅲc、Ⅲd对A-549有较显著活性,IC50分别为15.9±0.9μmol/L、14.2±1.3μmol/L。

    Abstract:

    A series of title compounds(Ⅲa-Ⅲf) were synthesized via microwave-assisted by the yield of 79.6%-84.1%, with α-hydroxyphosphonate and bromo mono-saccharide intermediates as raw materials, alkaline ionic liquid [Bmim]OH as catalyst. Their structures were confirmed by IR, 1HNMR and 13CNMR, and their antiproliferative activities were evaluated in some tumor cell lines by MTT assay. Prelimi-nary results in bioactivity tests indicated that some title compounds exhibited better activity. Among them, compounds Ⅲa, Ⅲb containing the glucose group had better inhibition effect against SGC-7901 with IC50 values of 12.9 ± 0.9μmol/L, 14.3± 1.1μmol/L respectively, compounds Ⅲc, Ⅲd containing the galactose fragments showed remarkable activities against A-549 with IC50 values of 15.9 ± 0.9μmol/L and 14.2 ± 1.3 μmol/L respectively.

    参考文献
    相似文献
    引证文献
引用本文

杨家强.膦酸酯糖苷衍生物的合成与抗肿瘤活性[J].精细化工,2018,35(12):

复制
分享
文章指标
  • 点击次数:
  • 下载次数:
  • HTML阅读次数:
  • 引用次数:
历史
  • 收稿日期:2018-04-09
  • 最后修改日期:2018-06-11
  • 录用日期:2018-06-14
  • 在线发布日期: 2018-11-08
  • 出版日期: