Fang Y, Tian S L, Li K Q, Zhao S W, Wang Z Y
National Institutes of Pharmaceutical Research & Development, Beijing.
Yao Xue Xue Bao. 1993;28(12):931-5.
In order to search for new compounds with higher anti-cancer activities and lower toxicities, 18 dehydrogenated carboncyclic analogs of norcantharidin, of which 17 are unknown compounds, were designed and synthesized. Preliminary screening results revealed that compound V6, VI1 and VI4 exhibited fairly apparent inhibitory activity against the growth of human-hepatoma cells, Bel-7402, in vitro. The inhibitory rate of VI4 is 52%, almost the same as that of norcantharidin, in the concentration of 0.05 mumol/ml.
为了寻找具有更高抗癌活性和更低毒性的新化合物，设计并合成了18种去氢碳环斑蝥素类似物，其中17种为未知化合物。初步筛选结果显示，化合物V6、VI1和VI4在体外对人肝癌细胞Bel-7402的生长表现出相当明显的抑制活性。在浓度为0.05μmol/ml时，VI4的抑制率为52%，几乎与斑蝥素相同。
