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Combretastatin 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

发表时间:2015-09-15  浏览量:1448  下载量:618
全部作者: 刘坤,朱启华,徐云根
作者单位: 中国药科大学药物化学教研室
摘 要: 为改善血管阻断剂Combretastatin A-4(CA-4)的水溶性和成药性,以戊二酰基为连接臂将CA-4与氨基糖进行偶联,设计合成6个CA-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1×10^5,1×10^6,1×10^7 mol/L 3个浓度对人脐静脉内皮细胞(human umbilical vein endothelial cells,HUVECs)增殖均有较强的抑制作用,其中化合物12d在1×10^5 mol/L和12f在1×10^7 mol/L浓度下对HUVECs抑制作用较阳性药CA-4更强。
关 键 词: 药物化学;血管生成抑制剂;Combretastatin A-4;氨基糖;偶联物
Title: Synthesis and inhibitory activity on human umbilical vein endothelial cells of mutual prodrug of Combretastatin A-4 and aminosaccharides
Author: LIU Kun, ZHU Qihua, XU Yungen
Organization: Department of Medicinal Chemistry, China Pharmaceutical University
Abstract: To improve the solubility and druggability of Combretastatin A-4 (CA-4), six coupling compounds (12a-12f) of CA-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 on the concentration of 1×10^5, 1×10^6, 1×10^7 mol/L could inhibit human umbilical vein endothelial cells (HUVECs) proliferation well in vitro. The inhibitory effects of 12d and 12f were more potent than positive drug Combretastatin A-4 at the concentration 1×10^5 mol/L and 1×10^7 mol/L respectively.
Key words: medicinal chemistry; angiogenesis inhibitor; Combretastatin A-4; aminosaccharides; mutual prodrug
发表期数: 2015年9月第17期
引用格式: 刘坤,朱启华,徐云根. Combretastatin 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[J]. 中国科技论文在线精品论文,2015,8(17):1844-1850.
 
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