Journal
CHEMICAL & PHARMACEUTICAL BULLETIN
Volume 55, Issue 7, Pages 1024-1029Publisher
PHARMACEUTICAL SOC JAPAN
DOI: 10.1248/cpb.55.1024
Keywords
Aspergillus fumigatus; semisynthesis; hydroxyethoxycinnamoyl fumagillol derivative; antiangiogenic activity; TNP-470
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A series of fumagillin analogues containing the C6-substituted cinnamoyl moiety were designed, synthesized, and evaluated for antiangiogenic activity. Among them, 4-hydroxyethoxy-cinnamoyl fumagillol (4a) and 4-hydroxyethoxy-3,5-dimethoxycinnamoyl fumagillol (4d) exhibited more potent anti-proliferation activity in CPAE and HUVEC cells with low cytotoxicity in vitro. These compounds are presently under further pharmacological evaluation studies.
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