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XIN Min-hang, XIANG Hua, SI Wen-bo, ZHAO Wei, XIAO Hong, YOU Qi-dong. Synthesis and antiangiogenic properties of 2-methoxestradiol-RGD peptide conjugates[J]. Journal of China Pharmaceutical University, 2011, 42(3): 198-205.
Citation: XIN Min-hang, XIANG Hua, SI Wen-bo, ZHAO Wei, XIAO Hong, YOU Qi-dong. Synthesis and antiangiogenic properties of 2-methoxestradiol-RGD peptide conjugates[J]. Journal of China Pharmaceutical University, 2011, 42(3): 198-205.
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Synthesis and antiangiogenic properties of 2-methoxestradiol-RGD peptide conjugates

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  • 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.
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