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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。
Aim To synthesize carboline derivatives and study their antitumor activity. Methods The α-carbolines, β-carbolines and 1,2,3,4-tetrahydro-β-carboline-3-carboxylic acids were used as starting materials to obtain 6- 6-substituted β-carbolines and 3-substituted β-carboline derivatives, MTT assay of the target compound on tumor cells. Results Fifteen novel carboline derivatives were synthesized and confirmed by 1H NMR and ESI-MS. Conclusion The target compounds obtained by MTT assay showed some antitumor activity against both tested cell lines and some compounds showed comparable or better tumor cell inhibitory activity than the positive control paclitaxel.