摘要
选择有机磷基团对斑蝥素的结构骨架进行修饰改造，以外式双环［２．２．１］庚－５－烯－２，３－二甲酸酐为原料，设计合成了一系列斑蝥素类似物．化合物的结构经１Ｈ ＮＭＲ， ＭＳ及元素分析确证．
Cantharidin, the active constituent of Mylabris, has displayed significant antitumor activities in vitro and in vivo. The adverse effects on urinary and gastrointestinal tracts prevent it from being accepted by the clinic. In order to search for new antitumor drugs with a high activity and low toxicity, a series of phosphonodipeptide derivatives of exo-bicyclo[2.2.1]heptane (or hept-5-ene )-2, 3-dicarboxylic anhydride were synthesized by the condensation of the corresponding amino acid derivatives of exo-bicyclo[2. 2. 1] hept-5-ene-2, 3-dicarboxylic anhydride with a-aminoalkylphosphonate, and their structures were confrimed by 1H NMR, MS and elemental analysis.
出处
《高等学校化学学报》
SCIE
EI
CAS
CSCD
北大核心
2000年第5期721-724,共4页
Chemical Journal of Chinese Universities
基金
国家自然科学基金!(批准号:29572053)
关键词
斑蝥素
膦二肽
合在
中草药
抗肿瘤药
Cantharidin
exo-Bicyclo[2.2.1]hept-5-ene-2
3-dicarboxylic anhydride
Phosphonodipeptide
