| 5-氨基-1,3-二氢-1,3-二氧-异吲哚-2-丙酸类衍生物的合成及抗血管生成活性研究 |
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| 引用本文： | 吴贝,杨大成,沈怡,邓勇,钟裕国.5-氨基-1,3-二氢-1,3-二氧-异吲哚-2-丙酸类衍生物的合成及抗血管生成活性研究[J].有机化学,2007,27(9):1110-1115. |
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| 作者姓名： | 吴贝 杨大成 沈怡 邓勇 钟裕国 |
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| 作者单位： | 1. 四川大学华西药学院靶向药物教育部重点实验室,成都,610041
2. 西南大学化学化工学院,重庆,400715 |
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| 基金项目： | 国家自然科学基金（No.20672077）资助项目. |
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| 摘 要： | 根据RGD序列肽的构效关系, 设计并合成了一系列以5-氨基-1,3-二氢-1,3-二氧-异吲哚-2-丙酸为分子骨架的新化合物. 其中间体和目标物的化学结构经1H NMR, MS和元素分析确证. 体外初步生物活性筛选结果表明, 目标物在10－5 mol/L浓度下对bFGF诱导的鸡胚绒毛尿囊膜新生血管生成有显著抑制活性.
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| 关 键 词： | RGD序列肽 5-氨基-1 3-二氢-1 3-二氧-异吲哚衍生物 合成 抗新生血管生成 |
| 收稿时间： | 2006-6-5 |
| 修稿时间： | 2006-06-062006-09-25 |
Synthesis of 5-Amino-1,3-dihydro-1,3-dioxo-isoindole-2-propanoic Acid Derivatives and Their Antiangiogenic Activities |
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| WU,Bei,YANG,Da-Cheng,SHEN,Yi,DENG,Yong,ZHONG,Yu-Guo.Synthesis of 5-Amino-1,3-dihydro-1,3-dioxo-isoindole-2-propanoic Acid Derivatives and Their Antiangiogenic Activities[J].Chinese Journal of Organic Chemistry,2007,27(9):1110-1115. |
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| Authors: | WU Bei YANG Da-Cheng SHEN Yi DENG Yong ZHONG Yu-Guo |
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| Institution: | 1 Key Laboratory of Drug Targeting, Ministry of Education, West China School of Pharmacy, Sichuan University, Chengdu 610041;2.School of Chemistry and Chemical Engineering, Southwest University, Chongqing 400715 |
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| Abstract: | Based on the structure-activity relationships of RGD-containing peptides,a series of novel 5-amino-1,3-dihydro-1,3-dioxo-isoindole derivatives were designed and synthesized.The intermediates and target compounds were characterized by 1H NMR,MS spectra and elemental analysis.Their ability to inhibit angiogenesis was evaluated in the chick embryo chorioallantoic membrane assay at 10-5 mol/L.Some com-pounds displayed obviously antiangiogenic activity induced by basic fibroblast growth factor. |
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| Keywords: | RGD sequence peptide 5-amino-1 3-dihydro-1 3-dioxo-isoindole derivative synthesis antian-giogenic |
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