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.
Publication types
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Alkaloids / chemical synthesis
-
Alkaloids / chemistry
-
Alkaloids / pharmacology
-
Carbazoles / chemical synthesis
-
Carbazoles / chemistry*
-
Carbazoles / pharmacology*
-
Cell Proliferation / drug effects
-
HeLa Cells
-
Humans
-
Inhibitory Concentration 50
-
Kinesins / antagonists & inhibitors*
-
Kinesins / metabolism
-
Mitosis / drug effects
-
Spindle Apparatus / drug effects
-
Spindle Apparatus / metabolism
-
Structure-Activity Relationship
Substances
-
Alkaloids
-
Carbazoles
-
KIF11 protein, human
-
Kinesins