Synthesis and anti-migrative evaluation of moverastin derivatives

Masato Sawada, Shin Ichiro Kubo, Koji Matsumura, Yasushi Takemoto, Hiroki Kobayashi, Etsu Tashiro, Takeshi Kitahara, Hidenori Watanabe, Masaya Imoto

Research output: Contribution to journalArticle

18 Citations (Scopus)

Abstract

Cell migration of tumor cells is essential for invasion of the extracellular matrix and for cell dissemination. Inhibition of the cell migration involved in the invasion process represents a potential therapeutic approach to the treatment of tumor metastasis; therefore, a novel series of derivatives of moverastins (moverastins A and B), an inhibitor of tumor cell migration, was designed and chemically synthesized. Among these moverastin derivatives, several compounds showed stronger cell migration inhibitory activity than parental moverastins, and UTKO1 was found to have the most potent inhibitory activity against the migration of human esophageal tumor EC17 cells in a chemotaxis cell chamber assay. Interestingly, although moverastins are considered to inhibit tumor cell migration by inhibiting farnesyltransferase (FTase), UTKO1 did not inhibit FTase, indicating that UTKO1 inhibited tumor cell migration by a mechanism other than the inhibition of FTase.

Original languageEnglish
Pages (from-to)1385-1389
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume21
Issue number5
DOIs
Publication statusPublished - 2011 Mar 1

Keywords

  • Cell migration
  • Chemical synthesis
  • UTKO1

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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  • Cite this

    Sawada, M., Kubo, S. I., Matsumura, K., Takemoto, Y., Kobayashi, H., Tashiro, E., Kitahara, T., Watanabe, H., & Imoto, M. (2011). Synthesis and anti-migrative evaluation of moverastin derivatives. Bioorganic and Medicinal Chemistry Letters, 21(5), 1385-1389. https://doi.org/10.1016/j.bmcl.2011.01.028