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

研究成果: Article査読

19 被引用数 (Scopus)

抄録

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.

本文言語English
ページ(範囲)1385-1389
ページ数5
ジャーナルBioorganic and Medicinal Chemistry Letters
21
5
DOI
出版ステータスPublished - 2011 3 1

ASJC Scopus subject areas

  • 生化学
  • 分子医療
  • 分子生物学
  • 薬科学
  • 創薬
  • 臨床生化学
  • 有機化学

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