Article

3-(3-Phenoxybenzyl)amino-β-carboline: a novel antitumor drug targeting α-tubulin.

Department of Pure and Applied Chemistry, Faculty of Science and Technology, Tokyo University of Science (RIKADAI), Noda, Chiba 278-8510, Japan.
Bioorganic & medicinal chemistry letters (impact factor: 2.65). 08/2011; 21(16):4784-7. DOI:10.1016/j.bmcl.2011.06.061 pp.4784-7
Source: PubMed

ABSTRACT 3-(3-Phenoxybenzyl)amino-β-carboline 2h showed extremely-high activity; the IC(50) value was 0.074 μM. To verify 2h-induced cell death types, we observed the chromatin condensation, the DNA fragmentation and activated caspase-3 using Hoechst 33342, agarose electrophoresis and western blot, and suggesting 2h-induced cell death type was apoptosis. Flow cytometry showed that 2h-treated cell was induced SubG1 cell population after G2/M cell cycle arrest. In addition, using affinity chromatography and peptide mass fingerprinting, we found that interacting protein with this compound was α-tubulin protein.

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Keywords

2h-induced cell death type
 
2h-treated cell
 
agarose electrophoresis
 
chromatin condensation
 
DNA fragmentation
 
extremely-high activity
 
peptide mass fingerprinting
 
verify 2h-induced cell death types