Synthesis and antiangiogenic properties of 2-methoxestradiol-RGD peptide conjugates / 中国药科大学学报

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.