论文部分内容阅读
目的:研究藤黄酸的构效关系。方法:通过对天然产物藤黄酸的结构剖析,在去除复杂桥环结构的基础上,合成了色酮和?酮2个系列的化合物。并通过MTT法对其进行了初步的药理实验活性筛选。结果:这些具有平面环结构的小分子化合物的活性虽然比藤黄酸的活性要低,但是引入异戊烯基能显著提高其抗肿瘤活性。结论:藤黄酸结构中的异戊烯基和桥环结构对其抗肿瘤活性有着很重要的作用。
Objective: To study the structure-activity relationship of gambogic acid. Methods: Based on the analysis of the structure of natural product gambogic acid, two series of compounds of chromone and ketone were synthesized based on the removal of the complex bridge structure. The preliminary pharmacological activity screening was performed by MTT method. Results: Although the activity of these small molecule compounds with a planar ring structure is lower than that of gambogic acid, the introduction of isopentenyl can significantly increase its antitumor activity. Conclusion: The isopentenyl and bridged ring structure of gambogic acid plays an important role in its anti-tumor activity.