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  

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

作　　者：吴贝[1] 杨大成[2] 沈怡[1] 邓勇[1] 钟裕国[1] 

机构地区：[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

出　　处：《有机化学》2007年第9期1110-1115,共6页Chinese Journal of Organic Chemistry

基　　金：国家自然科学基金(No20672077)资助项目

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1HNMR,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10-5mol/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.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 IH NMR, MS spectra and elemental analysis. Their ability to inhibit angiogenesis was evaluated in the chick embryo chorioaUantoic membrane assay at 10^-5 mol/L. Some compounds displayed obviously antiangiogenic activity induced by basic fibroblast growth factor.

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 

分 类 号：TQ463.5[化学工程—制药化工]