2甲-氧基雌二醇-RGD肽缀合物的合成及其抗血管生成作用(英文)  

Synthesis and antiangiogenic properties of 2-methoxestradiol-RGD peptide conjugates

作　　者：辛敏行[1] 向华[1] 司文博[1] 赵维[1] 肖红[2] 尤启冬[1] 

机构地区：[1]中国药科大学药物化学教研室,南京210009 [2]南京医科大学附属南京脑科医院神经精神病理研究所,南京210029

出　　处：《中国药科大学学报》2011年第3期198-205,共8页Journal of China Pharmaceutical University

基　　金：supported by the International Science and Technology Cooperation Project of Jiangsu Province(No. BZ2008058)

摘　　要：以2-甲氧基雌二醇为先导物,将其3位和17位通过连接基团与RGD肽偶联,合成了一系列2甲-氧基雌二醇-RGD肽缀合物,其中13个化合物未见文献报道,结构经IR,MS及1H NMR确证,并采用细胞迁移划痕试验初步测定了6个目标缀合物的抗血管生成活性。结果显示,化合物26c表现出较强的活性,强于先导物2甲-氧基雌二醇,从而证明了其潜在的抗血管生成作用。A series of 2-methoxyestradiol（2-MeO-E2） RGD peptide conjugates with coupling RGD peptides to 3-position or 17-position of 2-MeO-E2 through space linker were synthesized.Their antiangiogenic properties were preliminarily evaluated by cell migration scratch assays against HUVECs.Compound 26c binding RGDV peptide showed the best inhibitory effect.In addition,all 2-MeO-E2 RGD peptide conjugates exhibited obvious activity.These results demonstrate that conjugates with RGD peptides represent a promising means for targeting angiogenesis in cancer therapy.

关 键 词：2甲-氧基雌二醇 RGD肽缀合物 抗血管生成作用 细胞迁移划痕试验 

分 类 号：R914.5[医药卫生—药物化学]