Design, synthesis, and biological evaluation of angiogenesis inhibitors: aromatic enone and dienone analogues of curcumin.
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.
Robinson
Thomas Philip
TP
Computational Center for Molecular Structure and Design, Department of Chemistry, University of Georgia, Athens 30602-2556, USA.
Ehlers
Tedman
T
Hubbard IV
Richard B
RB
Bai
Xianhe
X
Arbiser
Jack L
JL
Goldsmith
David J
DJ
Bowen
J Phillip
JP
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
D020533:Angiogenesis Inhibitors; D000970:Antineoplastic Agents; D007659:Ketones; D011090:Polyenes; D003474:Curcumin