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中文摘要：
纺锤体驱动蛋白（kinesin spindle protein，KSP）是有丝分裂过程中二极纺锤体形成和维持所必需的。抑制KSP的功能将导致细胞周期停滞和细胞编程性细胞死亡，并且不干扰微管的其他功能，因而可成为潜在的肿瘤治疗靶点。本文合成了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。
英文摘要：
Kinesin spindle protein （KSP/Eg5） is essential for the formation and maintenance of bipolar spindles during mitosis. Inhibition of this protein leads to cell cycle arrest and apoptosis without interfering other microtubule-dependent processes. Therefore, it is a potential target in cancer therapy. Here, a series of tetrahydro-β-carboline derivatives 5a - k were synthesized as kinesin spindle protein inhibitor. Their structures were confirmed with ^1H NMR, ESI-MS and elemental analysis. The synthesized compounds were evaluated for their inhibition of KSP.
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Design, synthesis and bioevaluation of dihydropyrazolo[3,4-b]pyridine and benzo[4,5]imidazo[1,2-a]py
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