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graveoline 和 graveolinine 衍生物的合成与评价及其具有的强效抗血管生成活性。

Synthesis and evaluation of graveoline and graveolinine derivatives with potent anti-angiogenesis activities.

机构信息

School of Pharmaceutical Sciences, Sun Yat-sen University, Waihuan East Road 132, Guangzhou 510080, China.

出版信息

Eur J Med Chem. 2010 Sep;45(9):3895-903. doi: 10.1016/j.ejmech.2010.05.043. Epub 2010 May 26.

DOI:10.1016/j.ejmech.2010.05.043
PMID:20554355
Abstract

A series of graveoline and graveolinine derivatives were synthesized. The biological results showed that most of graveoline derivatives possessed higher cytotoxicity and better inhibitive effect against the adhesion and migration of human umbilical vein endothelial cell (HUVEC) than graveolinine derivatives. Among these compounds, 8d was the most potent agents that also showed significant anti-angiogenesis activities in chick embryo chorioallantoic membrane (CAM) assay.

摘要

合成了一系列的格拉夫林和格拉夫林衍生物。生物实验结果表明，大多数格拉夫林衍生物比格拉夫林衍生物具有更高的细胞毒性和对人脐静脉内皮细胞（HUVEC）黏附和迁移的抑制作用。在这些化合物中，8d 是最有效的药物，在鸡胚尿囊膜（CAM）试验中也表现出显著的抗血管生成活性。

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