Betulinic and platanic acid derived amides were prepared and screened for their cytotoxic activity. All of the compounds were shown to be cytotoxic for a panel of human tumor cell lines, and especially apoptotic betulinic acid derived compounds 6, 8 and 19 showed low EC₅₀ values. Of special interest was a 4-isoquinolinyl amide of 3-O-acetyl-betulinic acid (compound 19), being the most cytotoxic compound of this series and holding EC₅₀ values as low as EC₅₀ = 1.48 μM (A375 melanoma cells) while being significantly less cytotoxic for non-malignant fibroblasts NIH 3T3 with a selectivity index of > 91.2. This finding parallels previous results obtained for SAA21, a augustic acid derived compound thus making the 4-isoquinolinyl moiety to a privileged scaffold.

制备了由Betulinic和platanic衍生的酰胺，并筛选了它们的细胞毒性活性。所有化合物显示出是细胞毒性对人肿瘤细胞系的面板，特别是细胞凋亡桦木酸衍生的化合物6，8和19显示出低的EC ₅₀值。特别令人感兴趣的是3- O-乙酰基-贝丁酸的4-异喹啉基酰胺（化合物19），是该系列中最具细胞毒性的化合物，其EC ₅₀值低至EC ₅₀= 1.48μM（A375黑色素瘤细胞），而对非恶性成纤维细胞NIH 3T3的细胞毒性明显降低，选择性指数> 91.2。该发现与先前从SAA21（一种由奥古酸衍生的化合物）获得的结果相似，从而使4-异喹啉基部分成为了一种特殊的支架。