4.7 Article

Kinesin Spindle Protein (KSP) Inhibitors with 2,3-Fused Indole Scaffolds

Journal

JOURNAL OF MEDICINAL CHEMISTRY
Volume 53, Issue 13, Pages 5054-5058

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/jm100476d

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Funding

  1. Ministry of Education, Culture, Sports, Science and Technology, Japan
  2. JSPS

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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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