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| Combretastatins类肿瘤血管阻断剂的构效关系研究 | |
| 引用本文： | 周 全,陈建伟,刘晓蓉. Combretastatins类肿瘤血管阻断剂的构效关系研究[J]. 药学与临床研究, 2012, 20(3): 190-192 |
| 作者姓名： | 周 全 陈建伟 刘晓蓉 |
| 作者单位： | 1. 南京中医药大学药学院,南京210046; 南京圣和药业有限公司,南京210038 2. 南京中医药大学药学院,南京,210046 3. 南京圣和药业有限公司,南京,210038 |
| 摘 要： | 目的:通过对Combretastatins类肿瘤血管阻断剂构效关系研究,筛选出有潜力成为新一代肿瘤血管阻断剂候选药物。方法:以CA4为先导化合物,合成了6个全新的CA4类似物,并对其进行体外抗肿瘤实验以及酶抑制的活性测试研究。结果:6个全新化合物具有不同程度的抑制人癌细胞株增殖的作用,其中以C002化合物体外抗肿瘤活性最强。结论:化合物C002体外抗肿瘤活性与CA4相当,有潜力成为新一代肿瘤血管阻断剂的候选药物。 |
| 关 键 词： | Combretastatins类 构效关系 体外抗肿瘤实验 酶抑制活性测试 |
| 收稿时间： | 2012-03-03 |
| 修稿时间： | 2012-03-20 |
Structure-activity Relationship Research of Tumor Blood Vessel Blocker Combretastatins |
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| ZHOU Quan,CHEN Jian-wei and LIU Xiao-rong. Structure-activity Relationship Research of Tumor Blood Vessel Blocker Combretastatins[J]. Pharmacertical and Clinical Research, 2012, 20(3): 190-192 | |
| Authors: | ZHOU Quan CHEN Jian-wei LIU Xiao-rong |
| Affiliation: | 1Nanjing University of Chinese Medicine,Nanjing 210046,China; 2Nanjing Sanhome Pharmaceutical Co.,Ltd.,Nanjing 210038,China |
| Abstract: | Objective: To study the synthesis and structure-activity relationship about the combretastatin analogues as tumor blood vessel blockers,and screen the potential drug candidate that will be a new generation of tumor blood vessel blockers.Methods: Based on CA4 as the leading compound,six new CA4 analogues were synthesized,and tested in vitro for their antitumor and vascular disrupting activities.Results: Six new compounds had different degrees of antitumor activities in vitro,among which compound C002 was the strongest.Conclusion: Compound C002 has in vitro antitumor activity comparable to CA4,has the potential to be a new drug candidate of tumor blood vessel blockers. |
| Keywords: | Combretastatin analogues Structure-activity relationship In vitro antitumor experiment Activity of enzyme inhibition testing |
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