摘要
斑蝥素(Ⅰ)是我国传统中药斑蝥抗肿瘤作用的有效成分,临床证明对肝癌有肯定的疗效,但有毒副作用,特别是对泌尿系统的刺激作用较大。去甲斑蝥素(Ⅱ)有与Ⅰ类似的抗癌活性,对早、中期肝癌疗效较好,且毒性较低。我国已有学者对Ⅰ和Ⅱ进行结构改造。并由此发现了一些新的抗肿瘤化合物。我们以去甲斑螯素为原型化合物、以近年来抗癌药物研究的一些新进展为指导,设计并合成了一系列Ⅱ的类似物和衍生物,以期寻找高效低毒的抗肿瘤化合物。本文报道去甲斑蝥素氨基酸衍生物的合成(见图1和2)和初步活性筛选结果。
In order to search for new compounds with higher anti-cancer activities and lower toxicities, 19 amino acid derivatives of norcantharidin, of which 16 are unknown compounds, were designed and synthesized. Preliminary screening results revealed that 2-(syn-exo-7-oxabicyclo [2. 2. 1] heptane-2, 3-dicarboxylic imido)-N-phenyl glutaramic acid exhibited a fairly apparent inhibitory activity against human-hepatoma cells in vitro (inhibitory rate 39.4% at 0.025 μtmol/ml).
出处
《药学学报》
CAS
CSCD
北大核心
1993年第11期870-875,共6页
Acta Pharmaceutica Sinica
基金
国家自然科学基金
关键词
抗癌药
去甲斑蝥素
氨基酸
Norcantharidin
Amino acid derivatives
Bel-4702
Anticancer activity
