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-proliferation activity in CPAE and HUVEC cells with low cytotoxicity in vitro. These compounds are presently under further pharmacological evaluation studies.
Lee
Hong Woo
HW
New Drug Research Laboratories, Chong Kun Dang Research Institute, Cheonan, South Korea. hwlee@ckdpharm.com
Cho
Chin Sung
CS
Kang
Sung Kwon
SK
Yoo
Yong Sang
YS
Shin
Jae Soo
JS
Ahn
Soon Kil
SK
D020533:Angiogenesis Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D002417:Cattle; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D003510:Cyclohexanes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D005231:Fatty Acids, Unsaturated / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D051379:Mice; D015394:Molecular Structure; D012717:Sesquiterpenes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
D020533:Angiogenesis Inhibitors; D000970:Antineoplastic Agents; D003510:Cyclohexanes; D005231:Fatty Acids, Unsaturated; D012717:Sesquiterpenes; C026211:fumagillin