title: Synthesis and anti-migrative evaluation of moverastin derivatives.
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.
authors.affiliation: Department of Biosciences and Informatics, Faculty of Science and Technology, Keio University, Kohoku-ku, Yokohama, Japan.
authors.forename: Masato
authors.initials: M
authors.lastname: Sawada
authors.forename: Shin-ichiro
authors.initials: S
authors.lastname: Kubo
authors.forename: Koji
authors.initials: K
authors.lastname: Matsumura
authors.forename: Yasushi
authors.initials: Y
authors.lastname: Takemoto
authors.forename: Hiroki
authors.initials: H
authors.lastname: Kobayashi
authors.forename: Etsu
authors.initials: E
authors.lastname: Tashiro
authors.forename: Takeshi
authors.initials: T
authors.lastname: Kitahara
authors.forename: Hidenori
authors.initials: H
authors.lastname: Watanabe
authors.forename: Masaya
authors.initials: M
authors.lastname: Imoto
mesh_terms: D001547:Benzaldehydes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002465:Cell Movement / Q000187:drug effects; D003512:Cyclohexanones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D014407:Tumor Cells, Cultured
chemical_list: D001547:Benzaldehydes; D003512:Cyclohexanones; C558668:UTKO1 compound; C508258:moverastin A