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新型卟啉苦马豆素衍生物的合成及抗肿瘤活性

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新型抗肿瘤药的研究越来越受到重视.本文将氨基卟啉或羟基卟啉、POCl3 和苦马豆素缩合,合成了7 种新型卟啉苦马豆素衍生物(1a~1g),并对其抗肿瘤活性进行了评价.结果表明:设计合成的衍生物 1a~1g对SGC-7901 和Eca-109 肿瘤细胞均具有抑制作用.衍生物 1c对SGC-7901 和Eca-109 细胞的IC50 分别为 1.77±0.14 μM和3.32±0.13 μM,抗癌活性明显优于苦马豆素.所有衍生物的结构均经核磁共振、质谱和元素分析表征.
Synthesis and Anticancer Activity of Novel Porphyrin-swainsonine Derivatives
New research into anticancer drugs is increasingly gaining attention.In this paper,seven new swainsonine derivatives(1a~1g)were synthesized by the condensation of aminoporphyrin or hy-droxyl porphyrin,POCl3 and swainsonine,and their antitumor activities were evaluated.The results showed that derivatives 1a~1g all had inhibitory effects on SGC-7901 and Eca-109 tumor cells.The IC50 of derivative 1c for SGC-7901 and Eca-109 cells was 1.77±0.14 μM and 3.32±0.13 μM,re-spectively,which clearly indicates superior anticancer activity compared to swainsonine.The structures of all derivatives were confirmed by nuclear magnetic resonance,mass spectrometry and elemental analysis.

swainsonineporphyrinanticancer activityporphyrin-swainsonine derivativessynthesis

张志辉、王淑勋

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石家庄四药有限公司,河北 石家庄 052165

苦马豆素 卟啉 抗癌活性 卟啉苦马豆素衍生物 合成

河北省重点研发计划项目

22372705D

2024

合成化学
四川省化学化工学会 中国科学院成都有机化学研究所

合成化学

CSTPCD
影响因子:0.42
ISSN:1005-1511
年,卷(期):2024.32(3)
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