Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 54, Issue 13, Pages 4839-4846Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm200448n
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Funding
- Targeted Protein Research Program
- Ministry of Education, Culture, Sports, Science and Technology, Japan
- JSPS
- Grants-in-Aid for Scientific Research [23390025, 22590067] Funding Source: KAKEN
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The kinesin spindle protein (KSP) is a mitotic kinesin involved in the establishment of a functional bipolar mitotic spindle during cell division. It is considered to be an attractive target for cancer chemotherapy with reduced side effects. Based on natural product scaffold-derived fused indole-based inhibitors and known biphenyl-type KSP inhibitors, various carboline and carbazole derivatives were synthesized and biologically evaluated. beta-Carboline and lactam-fused carbazole derivatives exhibited remarkably potent KSP inhibitory activity and mitotic arrest in prometaphase with formation of an irregular monopolar spindle. The planar tri- and tetracyclic analogs inhibited KSP ATPase in an ATP-competitive manner just like biphenyl-type inhibitors.
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