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ID: ALA1806388

Journal: Bioorg Med Chem Lett

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

Authors: Ikeda R, Kurosawa M, Okabayashi T, Takei A, Yoshiwara M, Kumakura T, Sakai N, Funatsu O, Morita A, Ikekita M, Nakaike Y, Konakahara T.

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.

CiteXplore: 21752645

DOI: 10.1016/j.bmcl.2011.06.061