新型四氢-β-咔啉衍生物作为KSP抑制剂的合成及其抗肿瘤活性
[Synthesis and antitumor activity of novel tetrahydro-beta-carboline derivatives as KSP inhibitors].
作者信息
Ruan Xiu-Qin, Chen Ming, Wu Wu-Tong, You Qi-Dong
机构信息
Key Laboratory of Carcinogenesis and Intervention of Jiangsu Province, China Pharmaceutical University, Nanjing 210009, China.
出版信息
Yao Xue Xue Bao. 2013 Jul;48(7):1119-23.
Inhibitors of kinesin spindle protein (KSP) are a promising class of anticancer agents that cause mitotic arrest and induce apoptosis of tumor cells. A series of novel tetrahydro-beta-carboline derivatives were synthesized as kinesin spindle protein inhibitor and evaluated as potential antitumor agents. All compounds showed promising KSP inhibitiory activity. Compounds 8 and 9 exhibited better antitumor activity (Lung/A549, Stomach/AGS) than CK0106023 with GI50/IC50 values (1.07/1.62 and 1.46/3.27 micromol x L(-1), 1.09/>10 and 1.22/6.33 micromol x L(-1), respectively).
驱动蛋白纺锤体蛋白（KSP）抑制剂是一类很有前景的抗癌药物，可导致有丝分裂停滞并诱导肿瘤细胞凋亡。合成了一系列新型四氢-β-咔啉衍生物作为驱动蛋白纺锤体蛋白抑制剂，并评估其作为潜在抗肿瘤药物的活性。所有化合物均表现出有前景的KSP抑制活性。化合物8和9表现出比CK0106023更好的抗肿瘤活性（肺/A549、胃/AGS），其GI50/IC50值分别为（1.07/1.62和1.46/3.27 μmol·L⁻¹、1.09/>10和1.22/6.33 μmol·L⁻¹）。
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