Design, Synthesis, and Antiangiogenic Effects of a Series of Potent Novel Fumagillin Analogues

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-prolifera...

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Veröffentlicht in:	Chemical & pharmaceutical bulletin 2007, Vol.55(7), pp.1024-1029
Hauptverfasser:	Lee, Hong Woo, Cho, Chin Sung, Kang, Sung Kwon, Yoo, Yong Sang, Shin, Jae Soo, Ahn, Soon Kil
Format:	Artikel
Sprache:	eng
Schlagworte:	Angiogenesis Inhibitors - chemical synthesis Angiogenesis Inhibitors - chemistry Angiogenesis Inhibitors - pharmacology Animals antiangiogenic activity Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Aspergillus fumigatus Cattle Cell Line, Tumor Cell Proliferation - drug effects Cyclohexanes - chemical synthesis Cyclohexanes - chemistry Cyclohexanes - pharmacology Dose-Response Relationship, Drug Drug Design Drug Screening Assays, Antitumor Fatty Acids, Unsaturated - chemical synthesis Fatty Acids, Unsaturated - chemistry Fatty Acids, Unsaturated - pharmacology Humans hydroxyethoxycinnamoyl fumagillol derivative Mice Molecular Structure semisynthesis Sesquiterpenes - chemical synthesis Sesquiterpenes - chemistry Sesquiterpenes - pharmacology Structure-Activity Relationship TNP-470
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Zusammenfassung:	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.
ISSN:	0009-2363 1347-5223
DOI:	10.1248/cpb.55.1024