Synthesis and biological evaluation of novel EG5 inhibitors

Chembiochem. 2005 Nov;6(11):2005-13. doi: 10.1002/cbic.200500168.

Abstract

Human Eg5 is a mitotic kinesin that is essential for bipolar spindle formation and maintenance during mitosis. Recently, the discovery of compounds that inhibit Eg5 and cause mitotic arrest has attracted great interest, due to their potential use as the next generation of antimitotics. Here, we present the synthesis and biological investigation of 3,4-dihydrophenylquinazoline-2(1H)-thiones as selective and potent Eg5 inhibitors.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Algorithms
  • Animals
  • Antimitotic Agents / metabolism
  • Antimitotic Agents / pharmacology
  • Chlorocebus aethiops
  • Humans
  • Inhibitory Concentration 50
  • Kinesin / antagonists & inhibitors*
  • Mitosis / drug effects
  • Molecular Structure
  • Quinazolines / metabolism
  • Quinazolines / pharmacology*
  • Thiones / metabolism
  • Thiones / pharmacology*

Substances

  • Antimitotic Agents
  • KIF11 protein, human
  • Quinazolines
  • Thiones
  • Kinesin