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有机化学
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有机化学 ›› 2007, Vol. 27 ›› Issue (9): 1110-1115. 上一篇    下一篇

研究论文

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

吴贝a，杨大成b，沈怡a，邓勇*,a，钟裕国a   

  1. (a四川大学华西药学院靶向药物教育部重点实验室 成都 610041)
    (b西南大学化学化工学院 重庆 400715)
  • 收稿日期:2006-06-05 修回日期:1900-01-01 发布日期:2007-08-30
  • 通讯作者: 邓勇

Synthesis of 5-Amino-1,3-dihydro-1,3-dioxo-isoindole-2-propanoic Acid Derivatives and Their Antiangiogenic Activities

WU Beia,YANG Da-Chengb,SHEN Yia,DENG Yong*,a,ZHONG Yu-Guoa   

  1. (a Key Laboratory of Drug Targeting, Ministry of Education, West China School of Phar-macy,
    Sichuan University, Chengdu 610041)
    (b School of Chemistry and Chemical Engineering, Southwest University, Chongqing 400715)
  • Received:2006-06-05 Revised:1900-01-01 Published:2007-08-30
  • Contact: DENG Yong

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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.

关键词: RGD序列肽, 5-氨基-1,3-二氢-1,3-二氧-异吲哚衍生物, 抗新生血管生成, 合成

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 compounds displayed obviously antiangiogenic activity induced by basic fibroblast growth factor.

Key words: synthesis, antiangiogenic, 5-amino-1,3-dihydro-1,3-dioxo-isoindole derivative, RGD sequence peptide