毛叶假鹰爪素C衍生物的合成与抗肿瘤活性评价  

Synthesis and Antitumor Activity Evalution of Desmosdumotin C Derivatives

作　　者：舒彦松[1,2] 张学辉[2] 向卓[3] 梁海[1,2] 吴久鸿[2] 

机构地区：[1]安徽医科大学研究生学院,安徽合肥230032 [2]解放军306医院药学部,北京100101 [3]第四军医大学药学院,陕西西安710032

出　　处：《解放军药学学报》2013年第5期403-406,共4页Pharmaceutical Journal of Chinese People's Liberation Army

基　　金：国家自然科学基金;No.30572212;81072546

摘　　要：目的设计并合成出一系列Desmosdumotin C衍生物并考察其抗肿瘤活性。方法以2,4,6-三羟基苯乙酮为原料合成一系列Desmosdumotin C衍生物,目标化合物经过1H-NMR、MS鉴定。采用SRB法对其抗肿瘤活性进行初步评价。结果与结论设计并合成了19个新化合物,初步的细胞活性实验表明,该系列衍生物大多具有肿瘤增殖抑制活性,且与先导物相当,其中3个化合物显示出良好的抗肿瘤活性,为进一步对先导化合物Desmosdumotin C衍生物的结构优化奠定了一定的基础。Objective To design and synthesize a series of Desmosdumotin C derivatives and screen their anti-tumor activity. Methods These compounds were prepared from 2,4, 6-trihydroxyacetophenone as starting agents. Their structures were indetified by 1H-NMR and MS. The anti-tumor activity of the compounds was screened by SRB methods. Results and Conclusion Nineteen novel compounds have been synthesized,three of which have better anti-tumor activities.

关 键 词：Desmosdumotin C衍生物 合成 抗肿瘤活性 

分 类 号：R914.5[医药卫生—药物化学]