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目的基于西松烷型二萜天然产物新巴豆瑞士松酸进行结构修饰,并对得到的衍生物进行体外抗肿瘤活性评价。方法以新巴豆瑞士松酸为起始原料,通过缩合反应、点击化学反应得到目标化合物。采用噻唑蓝(MTT)法考察所合成的目标化合物对HeLa、K562和K562A/02肿瘤细胞的抗增殖活性。结果合成了11个文献未报道的新巴豆瑞士松酸衍生物,其结构经~1H-NMR、~(13)C-NMR及HR-MS确定。活性测试结果表明,部分衍生物表现出一定的抗肿瘤活性,其中,化合物2f对HeLa细胞表现出良好活性,化合物2e对K562和耐药的K562A/02细胞表现出良好活性。结论部分衍生物对耐药的K562A/02细胞表现出抗肿瘤活性,具有进一步研究价值。
OBJECTIVE: To construct the structural modification of cedrol diterpenoid natural product cedarwood pimaric acid and to evaluate the antitumor activity of the obtained derivative in vitro. Methods New cordyceps kapok was used as the starting material and the target compound was obtained by the condensation reaction and click chemistry. The anti-proliferative activity of the target compounds on HeLa, K562 and K562A / 02 tumor cells was investigated by MTT assay. Results 11 novel cantharidin derivatives not reported in the literature were synthesized and their structures were confirmed by ~ 1H-NMR, ~ (13) C-NMR and HR-MS. The results of the activity test showed that some of the derivatives showed some anti-tumor activity, in which compound 2f showed good activity on HeLa cells and compound 2e showed good activity on K562 and resistant K562A / 02 cells. Conclusion Some of the derivatives showed anti-tumor activity on drug-resistant K562A / 02 cells, which has further research value.