Chemical Modification of Fumagillin. III. Modification of the Spiro-epoxide

Shogo MARUI; Toshihiro YAMAMOTO; Katsuichi SUDO; Hiroshi AKIMOTO; Shoji KISHIMOTO

doi:10.1248/cpb.43.588

Shogo MARUI, Toshihiro YAMAMOTO, Katsuichi SUDO, Hiroshi AKIMOTO, Shoji KISHIMOTO

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Keywords: fumagillin, AGM-1470, sulfonium analogue, anti-angiogenic activity, antitumor activity

JOURNAL FREE ACCESS

1995 Volume 43 Issue 4 Pages 588-593

DOI https://doi.org/10.1248/cpb.43.588

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Abstract

The spiro-epoxy group of fumagillol (2) was selectively modified and several analogues of AGM-1470 (3) with a (dialkyl)-β-hydroxyethylsulfonium moiety were prepared. These analogues were found to inhibit angiogenesis induced by basic fibroblast growth factor in the rat micropocket assay. They also inhibited the growth of M5076 cells in vivo, but did not affect the body weight change of the tested mice during the assay.

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