Bioorganic and Medicinal Chemistry Letters p. 1385 - 1389 (2011)
Update date:2022-08-05
Topics:
Sawada, Masato
Kubo, Shin-Ichiro
Matsumura, Koji
Takemoto, Yasushi
Kobayashi, Hiroki
Tashiro, Etsu
Kitahara, Takeshi
Watanabe, Hidenori
Imoto, Masaya
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.
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