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抗肿瘤药物研究Ⅰ:去甲斑蝥素氨基酸衍生物的合成与抗癌活性
引用本文:田少雷,赵树纬,朱爱堂,方茵,李克庆. 抗肿瘤药物研究Ⅰ:去甲斑蝥素氨基酸衍生物的合成与抗癌活性[J]. 药学学报, 1993, 28(11): 870-875
作者姓名:田少雷  赵树纬  朱爱堂  方茵  李克庆
作者单位:中国医药研究开发中心,中国医药研究开发中心,北京医科大学药化专业,中国医药研究开发中心,中国医药研究开发中心 北京 102206,北京 102206,86级实习生,北京 102206,北京 102206
摘    要:
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).

关 键 词:去甲斑蝥素  氨基酸衍生物  Bel-4702  抗癌活性
收稿时间:1992-11-21

STUDIES ON ANTI-TUMER AGENTS Ⅰ:SYNTHESIS AND ANTI-CANCER ACTIVITY OF AMINO ACID DERIVATIVES OF NORCANTHARIDIN
SL Tian,SW Zhao,AT Zhu,Y Fang and KQ Li. STUDIES ON ANTI-TUMER AGENTS Ⅰ:SYNTHESIS AND ANTI-CANCER ACTIVITY OF AMINO ACID DERIVATIVES OF NORCANTHARIDIN[J]. Acta pharmaceutica Sinica, 1993, 28(11): 870-875
Authors:SL Tian  SW Zhao  AT Zhu  Y Fang  KQ Li
Abstract:
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).
Keywords:Norcantharidin  Amino acid derivatives  Bel-4702  Anticancer activity
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