Combretastatins类肿瘤血管阻断剂的构效关系研究

摘要

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.%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.