| 2-甲氧基雌二醇-RGD肽缀合物的合成及其抗血管生成作用 |
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| 引用本文： | 辛敏行,向华,司文博,赵维,肖红,尤启冬.2-甲氧基雌二醇-RGD肽缀合物的合成及其抗血管生成作用[J].中国药科大学学报,2011,42(3):198-205. |
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| 作者姓名： | 辛敏行 向华 司文博 赵维 肖红 尤启冬 |
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| 作者单位： | 中国药科大学药物化学教研室;中国药科大学药物化学教研室;中国药科大学药物化学教研室;中国药科大学药物化学教研室;南京医科大学附属南京脑科医院神经精神病理研究所;中国药科大学药物化学教研室 |
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| 基金项目： | supported by the International Science and Technology Cooperation Project of Jiangsu Province(No. BZ2008058) |
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| 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。
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| 关 键 词： | 2-甲氧基雌二醇 RGD肽缀合物 抗血管生成作用 细胞迁移划痕试验 |
Synthesis and antiangiogenic properties of 2-methoxestradiol-RGD peptide conjugates |
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| XIN Min-hang,XIANG Hu,SI Wen-bo,ZHAO Wei,XIAO Hong and 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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| Authors: | XIN Min-hang XIANG Hu SI Wen-bo ZHAO Wei XIAO Hong and YOU Qi-dong |
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| Institution: | XIN Min-hang1,XIANG Hua1,SI Wen-bo1,ZHAO Wei1,XIAO Hong2,YOU Qi-dong1 1Department of Medical Chemistry,China Pharmaceutical University,Nanjing 210009,2Neuro-psychiatric Institute,Nanjing Brain Hospital,Nanjing Medical University,Nanjing 210029,China |
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| 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 fo... |
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| Keywords: | 2-methoxyestradiol RGD peptide conjugates antiangiogenic properties cell migration scratch assays |
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