CAJ | 학술논문

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.
목적:연구등황산적구효관계.방법:통과대천연산물등황산적결구부석,재거제복잡교배결구적기출상,합성료색동화동2개계렬적화합물.병통과MTT법대기진행료초보적약리실험활성사선.결과:저사구유평면배결구적소분자화합물적활성수연비등황산적활성요저,단시인입이무희기능현저제고기항종류활성.결론:등황산결구중적이무희기화교배결구대기항종류활성유착흔중요적작용.
AIM: To investigate the basic structure-activity relationship of gambogic acid. METHODS: Through simplifying the complex skeleton of the natural gambogic acid, two series of derivatives of chromone and xanthone were synthesized and examined for their antitumor activities against several cancer cells in vitro by MTT method. RESULTS: The cytotoxic activities of all these small compounds with planar ring were much less potent than those of the natural gambogic acid, and the introduction of prenyl to these small molecular compounds could increase their antitumor activities. CONCLUSION: The structure-activity relationship of synthesized compounds indicated that the prenyl groups and the bridgecore in gambogic acid were very important for keeping its antitumor activities.