title: Design, synthesis, and antiangiogenic effects of a series of potent novel fumagillin analogues.
abstract: 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.
authors.affiliation: New Drug Research Laboratories, Chong Kun Dang Research Institute, Cheonan, South Korea. hwlee@ckdpharm.com
authors.forename: Hong Woo
authors.initials: HW
authors.lastname: Lee
authors.forename: Chin Sung
authors.initials: CS
authors.lastname: Cho
authors.forename: Sung Kwon
authors.initials: SK
authors.lastname: Kang
authors.forename: Yong Sang
authors.initials: YS
authors.lastname: Yoo
authors.forename: Jae Soo
authors.initials: JS
authors.lastname: Shin
authors.forename: Soon Kil
authors.initials: SK
authors.lastname: Ahn
mesh_terms: 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
chemical_list: D020533:Angiogenesis Inhibitors; D000970:Antineoplastic Agents; D003510:Cyclohexanes; D005231:Fatty Acids, Unsaturated; D012717:Sesquiterpenes; C026211:fumagillin