Combretastatins类肿瘤血管阻断剂的构效关系研究

Structure-activity Relationship Research of Tumor Blood Vessel Blocker Combretastatins

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。

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.