ombretastatin A-4氨基糖偶联物的合成及其对人脐静脉内皮细胞增殖的抑制活性
Synthesis and inhibition of HUVECs proliferation of mutual prodrug of Combretastatin A-4 and glucosamines
为改善血管阻断剂Combretastatin A-4的水溶性和成药性，本文利用前药原理，以戊二酰基为连接臂，将Combretastatin A-4与氨基糖进行偶联，设计合成6个Combretastatin A-4氨基糖偶联物(12a~12f)，其结构经１H NMR、MS确证。体外药理实验结果显示6个目标化合物在10-5, 10-6, 10-7 mol/L三个浓度对人脐静脉内皮细胞增殖均有较强的抑制作用。其中化合物12d在10-5 mol/L和12f在10-7mol/L浓度下对人脐静脉内皮细胞抑制作用较阳性药Combretastatin A-4更强。
o improve the solubility and druggability of Combretastatin A-4, six coupling compounds (12a~12f) of Combretastatin A-4 and aminosaccharides were designed and synthesized. Their structures were characterized by 1H NMR, MS. Preliminary biological evaluation results showed that all the target compounds could inhibit HUVEC cell proliferation well in vitro.The inhibitory effects of 12d and 12f were more potent than positive drug Combretastatin A-4 at the concentration 10-5 mol/L and 10-7mol/L respectively.
徐云根、刘坤、朱启华
药学基础医学生物化学
药物化学ombretastatin A-4氨基糖偶联物血管生成抑制剂
Medicinal chemistryCombretastatin A-4aminosaccharidesmutual prodrugangiogenesis inhibitor
徐云根,刘坤,朱启华.ombretastatin A-4氨基糖偶联物的合成及其对人脐静脉内皮细胞增殖的抑制活性[EB/OL].(2014-05-06)[2025-08-02].http://www.paper.edu.cn/releasepaper/content/201405-73.点此复制
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