Development of tubulin-polymerization inhibitors based on the thalidomide skeleton

Hiroshi Aoyama, Tomomi Noguchi, Takashi Misawa, Takanori Nakamura, Hiroyuki Miyachi, Yuichi Hashimoto, Hisayoshi Kobayashi

Research output: Contribution to journalArticle

10 Citations (Scopus)

Abstract

We synthesized a series of compounds based on the potent tubulin-polymerization inhibitor 5-hydroxy-2-(2,6-diisopropylphenyl)-1H- isoindole-1,3-dione [5HPP-33 (3)], which is structurally derived from thalidomide (1), and investigated their inhibitory effects on tubulin polymerization. Direct interaction between 5HPP-33 (3) and α,β- tubulin heterodimer protein was demonstrated by means of a surface plasmon resonance study.

Original languageEnglish
Pages (from-to)944-949
Number of pages6
JournalChemical and Pharmaceutical Bulletin
Volume55
Issue number6
DOIs
Publication statusPublished - Jun 1 2007

Keywords

  • Phthalimide skeleton
  • Surface plasmon resonance
  • Thalidomide
  • Tubulin polymerization inhibitor

ASJC Scopus subject areas

  • Chemistry(all)
  • Drug Discovery

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    Aoyama, H., Noguchi, T., Misawa, T., Nakamura, T., Miyachi, H., Hashimoto, Y., & Kobayashi, H. (2007). Development of tubulin-polymerization inhibitors based on the thalidomide skeleton. Chemical and Pharmaceutical Bulletin, 55(6), 944-949. https://doi.org/10.1248/cpb.55.944