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纺锤体驱动蛋白(kinesin spindle protein,KSP)的功能被抑制将导致细胞周期停滞和细胞编程性细胞死亡,因而可成为潜在的肿瘤治疗靶点。本文合成了10个新的β-四氢咔啉衍生物,化合物结构经元素分析、IR、1H NMR和质谱确证。生物活性测试结果表明目标化合物具有一定的KSP抑制活性,体外抗肿瘤活性测试结果显示,化合物8和9对肿瘤细胞Lung/A549的GI50/IC50分别为1.07/1.62和1.46/3.27μmol.L 1,对Stomach/AGS的GI50/IC50分别为1.09/>10和1.22/6.33μmol.L 1,抗增殖活性优于阳性对照物CK0106023。
Inhibition of the function of kinesin spindle protein (KSP) leads to cell cycle arrest and apoptosis, which may be potential targets for oncology treatment. In this paper, 10 new β-tetrahydrocarboline derivatives were synthesized. Their structures were confirmed by elemental analysis, IR, 1H NMR and mass spectra. The results of biological activity test showed that the target compound had certain KSP inhibitory activity. The in vitro antitumor activity test showed that the compound of compound 8 and 9 had GI50 / IC50 of 1.07 / 1.62 and 1.46 / 3.27μmol.L 1, respectively, for Lung / A549 tumor cells, The GI50 / IC50 of Stomach / AGS was 1.09 /> 10 and 1.22 / 6.33μmol.L 1, respectively. The antiproliferative activity was better than the positive control CK0106023.