二肽类膦酸酯衍生物的合成与抗肿瘤活性

吴学姣 苟光淋 杨小兰 杨家强

引用本文: 吴学姣, 苟光淋, 杨小兰, 杨家强. 二肽类膦酸酯衍生物的合成与抗肿瘤活性[J]. 应用化学, 2021, 38(1): 36-43. doi: 10.19894/j.issn.1000-0518.200183 shu
Citation:  WU Xue-Jiao,  GOU Guang-Lin,  YANG Xiao-Lan,  YANG Jia-Qiang. Synthesis and Antitumor Activity of Phosphonate Derivatives Containing Dipeptide[J]. Chinese Journal of Applied Chemistry, 2021, 38(1): 36-43. doi: 10.19894/j.issn.1000-0518.200183 shu

二肽类膦酸酯衍生物的合成与抗肿瘤活性

    通讯作者: 杨家强,E-mail:yjqcn@126.com
  • 基金项目:

    贵州省科技厅国际合作项目(No.黔科合外G字[2014]7013)资助

摘要: 为了寻找抗肿瘤活性化合物,以前期研究的含一个氨基酸结构单元的膦酸酯衍生物为基础,设计合成了15个二肽类膦酸酯衍生物(Ⅲa-Ⅲo)。采用溴化噻唑蓝四氮唑(MTT)法进行体外抗肿瘤活性测试。结果表明:该类化合物对人肺癌细胞(A-549)、人胃癌细胞(SGC-7901))和人食管癌细胞(EC-109)有潜在增殖抑制作用。其中,化合物Ⅲf对A-549和EC-109的半数抑制浓度(IC50)分别为(6.9±1.2)和(6.3±1.0)μmol/L,化合物Ⅲn对SGC-7901和EC-109的IC50分别为(6.7±1.0)和(6.1±1.0)μmol/L,与对照药顺铂接近。

English


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  • 收稿日期:  2020-06-14
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