2-甲氧基雌二醇-RGD肽缀合物的合成及其抗血管生成作用

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

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。

Abstract: 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-E₂ RGD peptide conjugates exhibited obvious activity.These results demonstrate that conjugates with RGD peptides represent a promising means for targeting angiogenesis in cancer therapy.