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

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

  • Bioorg Med Chem Lett. 2011 Aug 15;21(16):4784-7. doi: 10.1016/j.bmcl.2011.06.061.
Reiko Ikeda 1,  Masaki Kurosawa,  Takazumi Okabayashi,  Ayako Takei,  Masamichi Yoshiwara,  Tadashi Kumakura,  Norio Sakai,  Osamu Funatsu,  Akinori Morita,  Masahiko Ikekita,  Yumi Nakaike,  Takeo Konakahara
Affiliations

Affiliation

  • 1 Department of Pure and Applied Chemistry, Faculty of Science and Technology, Tokyo University of Science (RIKADAI), Noda, Chiba 278-8510, Japan.
PMID: 21752645 DOI: 10.1016/j.bmcl.2011.06.061
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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