作者:Shinya Oishi、Toshiaki Watanabe、Jun-ichi Sawada、Akira Asai、Hiroaki Ohno、Nobutaka Fujii
DOI:10.1021/jm100476d
日期:2010.7.8
On the basis of a common 2,3-fused indole substructure within the complex frameworks of terpendole E and other KSP inhibitors, the carbazoles with a bulky alkyl group were identified as a novel KSP inhibitory scaffold. Additionally, among several naturally occurring cell growth inhibitors with 2,3-fused indole structures, β-carboline alkaloids, harman and harmine, showed moderate inhibition of KSP
有丝分裂驱动蛋白纺锤体蛋白(KSP)在细胞分裂过程中参与了双极纺锤体的组装。根据萜烯E和其他KSP抑制剂复杂框架中常见的2,3-稠合的吲哚亚结构,具有庞大烷基的咔唑被鉴定为新型KSP抑制支架。另外,在具有2,3-融合的吲哚结构的几种天然存在的细胞生长抑制剂中,β-咔啉生物碱,harman和harmine显示出对KSP的中等抑制作用。