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中文摘要：
纺锤体驱动蛋白（kinesin spindle protein，KSP／Eg5）作为潜在的肿瘤治疗靶点，使发现KSP抑制剂成为热点．设计并合成了4-氧基-β-四氢咔啉衍生物作为新型的KSP抑制剂，并测定了其对KSP的抑制活性，均优于阳性对照物．其中化合物9c抑制KSP的IC50=0．065umol·L^-1，优于阳性对照物Monastrol 100多倍．生物活性研究表明为抗肿瘤药物提供了新结构类型的候选化合物．
英文摘要：
The kinesin spindle protein （KSP/Eg5） is a potential target in cancer therapy, which has attracted great interest in discovery of compounds that inhibit KSP. Here, a series of 4-oxo-tetrahydro-β-carline derivatives 9a-9f have been designed and synthesized as a novel class of KSP inhibitor, and evaluated for their inhibition aganist KSP. All compounds inhibited ATPase activity with ICs0 below that of the analog Monastrol. 9c has an IC50=0.065 umolo·L^-1 for inhibition of KSP, 〉 100-fold more active than Monastrol. The research results provide new candidate molecules for study of anticancer drugs.
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