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

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

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 i...

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Veröffentlicht in:Chemical & pharmaceutical bulletin 1995/04/15, Vol.43(4), pp.588-593
Hauptverfasser: MARUI, Shogo, YAMAMOTO, Toshihiro, SUDO, Katsuichi, AKIMOTO, Hiroshi, KISHIMOTO, Shoji
Format: Artikel
Sprache:eng
Schlagworte:
AGM-1470
anti-angiogenic activity
Antineoplastic agents
antitumor activity
Biological and medical sciences
fumagillin
General aspects
Medical sciences
Pharmacology. Drug treatments
sulfonium analogue
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Zusammenfassung: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.
ISSN:0009-2363
1347-5223
DOI:10.1248/cpb.43.588