新型四氢-β-咔啉作为有丝分裂驱动蛋白Eg5抑制剂的合成及生物学评价
Synthesis and biological evaluation of new tetrahydro-beta-carbolines as inhibitors of the mitotic kinesin Eg5.
作者信息
Sunder-Plassmann Nils, Sarli Vasiliki, Gartner Michael, Utz Mathias, Seiler Jeanette, Huemmer Stefan, Mayer Thomas U, Surrey Thomas, Giannis Athanassios
机构信息
University of Leipzig, Institute for Organic Chemistry, Johannisallee 29, 04103 Leipzig, Germany.
出版信息
Bioorg Med Chem. 2005 Nov 15;13(22):6094-111. doi: 10.1016/j.bmc.2005.06.027. Epub 2005 Aug 3.
The mitotic kinesin Eg5 (or KSP) is a crucial player in the development and function of the mitotic spindle. Inhibition of this protein leads to cell cycle arrest and apoptosis without interfering with other microtubule-dependent processes. Therefore, it is a potential target in cancer therapy. Here, we report the synthesis and biological evaluation of a small library of molecules based on the structure of the known Eg5 inhibitor HR22C16. One of these derivatives (compound trans-24) proved to be a potent and specific Eg5 inhibitor.
有丝分裂驱动蛋白Eg5（或KSP）在有丝分裂纺锤体的发育和功能中起着关键作用。抑制这种蛋白质会导致细胞周期停滞和凋亡，而不会干扰其他依赖微管的过程。因此，它是癌症治疗中的一个潜在靶点。在此，我们报告基于已知Eg5抑制剂HR22C16的结构合成并生物学评估了一个小分子文库。这些衍生物之一（化合物反式-24）被证明是一种有效的、特异性的Eg5抑制剂。
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