Synthesis and antiangiogenic properties of 2-methoxestradiol-RGD peptide conjugates
- VernacularTitle:2-甲氧基雌二醇-RGD肽缀合物的合成及其抗血管生成作用
- Author:
Minhang XIN
;
Hua XIANG
;
Wenbo SI
;
Wei ZHAO
;
Hong XIAO
;
Qidong YOU
- Publication Type:Journal Article
- Keywords:
2-methoxyestradiol;
RGD peptide conjugates;
antiangiogenic properties;
cell migration scratch assays
- From:
Journal of China Pharmaceutical University
2011;42(3):198-205
- CountryChina
- Language:Chinese
-
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-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.
