title: Design, synthesis, and biological evaluation of angiogenesis inhibitors: aromatic enone and dienone analogues of curcumin.
abstract: The quest to find new antitumor compounds is an ongoing research endeavor in many laboratories around the world. The use of small-molecule angiogenesis inhibitors promises to be a potentially effective method for cancer treatment and possible prevention. Many antiangiogenic compounds are in various stages of laboratory evaluations and clinical trials. Curcumin is a natural product that has exhibited potent antiangiogenic properties. Based on a simple pharmacophore model, using standard drug design concepts, aromatic enone and aromatic dienone analogues of curcumin were prepared and/or obtained commercially. These compounds were screened for antiangiogenic properties via an in vitro SVR assay and were found to inhibit cell proliferation.
authors.affiliation: Computational Center for Molecular Structure and Design, Department of Chemistry, University of Georgia, Athens 30602-2556, USA.
authors.forename: Thomas Philip
authors.initials: TP
authors.lastname: Robinson
authors.forename: Tedman
authors.initials: T
authors.lastname: Ehlers
authors.forename: Richard B
authors.initials: RB
authors.lastname: Hubbard IV
authors.forename: Xianhe
authors.initials: X
authors.lastname: Bai
authors.forename: Jack L
authors.initials: JL
authors.lastname: Arbiser
authors.forename: David J
authors.initials: DJ
authors.lastname: Goldsmith
authors.forename: J Phillip
authors.initials: JP
authors.lastname: Bowen
mesh_terms: D020533:Angiogenesis Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology; D002455:Cell Division / Q000187:drug effects; D002461:Cell Line, Transformed; D003474:Curcumin / Q000031:analogs & derivatives* / Q000138:chemical synthesis; D015195:Drug Design; D004730:Endothelium, Vascular / Q000166:cytology; D007659:Ketones; D051379:Mice; D011090:Polyenes; D013329:Structure-Activity Relationship
chemical_list: D020533:Angiogenesis Inhibitors; D000970:Antineoplastic Agents; D007659:Ketones; D011090:Polyenes; D003474:Curcumin