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Jaspine B是从海绵中提取的具有显著肿瘤活性的天然产物.为了寻找活性更好,合成方法更简洁的抗肿瘤化合物,设计并合成了一系列3-epi-Jaspine B类似物,共16个化合物,所合成的化合物均未见文献报道.所有化合物都经过~1H NMR、~(13)C NMR和HRMS确定分子结构.对所合成的化合物用噻唑蓝(MTT)法对4种肿瘤细胞(B16-F10小鼠皮肤黑色素瘤细胞、A-549人肺癌细胞、MCF-7人乳腺癌细胞、PC-3人前列腺癌细胞)进行生物活性测试,部分化合物对肿瘤细胞有抑制作用,其中化合物8f和11对A-549人肺癌细胞具有较好的活性,其IC_(50)分别为(9.646±0.984)和(7.144±0.854)μg/m L.
Jaspine B is a natural product extracted from sponge with significant tumor activity.In order to find a more active and more concise anti-tumor compound, a series of 3-epi-Jaspine B analogues were designed and synthesized, a total of 16 compounds , All of the synthesized compounds have not been reported in the literature.All the compounds were confirmed by 1H NMR, 13 C NMR and HRMS.The compounds were analyzed by MTT assay for four kinds of tumor cells (B16 -F10 mouse cutaneous melanoma cells, A-549 human lung cancer cells, MCF-7 human breast cancer cells and PC-3 human prostate cancer cells). Some of the compounds showed inhibitory effects on tumor cells. Compounds 8f and 11 had good activity on A-549 human lung cancer cells with IC 50 of (9.646 ± 0.984) and (7.144 ± 0.854) μg / m L, respectively.