咔啉类衍生物的合成及抗肿瘤活性研究  

Synthesis and Antitumor Activity Study of Carboline Derivatives

作　　者：陈静[1] 陶雪芬[1] 

机构地区：[1]浙江中医药大学药学院药物化学教研室,杭州310053

出　　处：《中国现代应用药学》2013年第3期229-234,共6页Chinese Journal of Modern Applied Pharmacy

基　　金：国家自然科学基金项目(81102315);高等学校博士学科点专项科研基金(20103322120002)

摘　　要：目的合成咔啉类衍生物并研究其抗肿瘤活性。方法以α-咔啉、β-咔啉以及1,2,3,4-四氢-β-咔啉-3-羧酸为原料,经过多步反应分别得到6-取代α-咔啉类、6-取代β-咔啉类以及3-取代β-咔啉类衍生物,用MTT法考察目标化合物对肿瘤细胞的抑制作用。结果合成了15个新的咔啉类衍生物,结构经过1H NMR和ESI-M S确证。结论 MTT法测试所得的目标化合物对2种受试细胞株均具有一定的抗肿瘤活性,部分化合物显示出与阳性对照紫杉醇相当或更佳的肿瘤细胞抑制活性。OBJECTIVE To synthesize a series of carboline derivatives and determine their antitumor activity. METHODS 6-Substituted-α-carboline derivatives, 6-substituted-β-carboline derivatives and 3-substituted-β-carboline derivatives were synthesized through several steps from α-carboline, β-carboline and 1,2,3,4-tetrahydro-β-carboline-3-carboxylic acid separately. The antitumor activities of the target compounds were studied by MTT method. RESULTS Fifteen novel carboline derivatives were synthesized and their structures were characterized by 1H NMR and ESI-MS. CONCLUSION All the target compounds showed antitumor activity against the tested tumor cells, some were comparable with that of taxol.

关 键 词：咔啉衍生物 合成 抗肿瘤活性 

分 类 号：R916.696[医药卫生—药学]