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

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.