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Kinesin spindle protein (KSP) inhibitors with 2,3-fused indole scaffolds
Shinya Oishi1, Toshiaki Watanabe, Jun-Ichi Sawada
1Graduate School of Pharmaceutical Sciences, Kyoto University, Sakyo-ku, Kyoto 606-8501, Japan. soishi@pharm.kyoto-u.ac.jp
Abstract:
Mitotic kinesin spindle protein (KSP) is involved in the assembly of the bipolar spindle during cell division. 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, beta-carboline alkaloids, harman and harmine, showed moderate inhibition of KSP.
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