Synthesis and biological evaluation of aromatic enones related to curcumin.
Curcumin, a natural product isolated from the spice turmeric, has been shown to exhibit a wide range of pharmacological activities including certain anti-cancer properties. It has been specifically shown to be an effective inhibitor of angiogenesis both in vitro and in vivo. Using curcumin as a lead compound for anti-angiogenic analog design, a series of structurally related compounds utilizing a substituted chalcone backbone have been synthesized and tested via an established SVR cell proliferation assay. The results have yielded a wide range of compounds that equal or exceed curcumin's ability to inhibit endothelial cell growth in vitro. Due to both their commercial availability and their fairly straightforward synthetic preparation, these low molecular weight compounds are attractive leads for developing future angiogenic inhibitors.
Robinson
Thomas Philip
TP
Center for Biomolecular Structure and Dynamics, Department of Chemistry, University of Georgia, Athens, GA 30602, USA.
Hubbard
Richard B
RB
Ehlers
Tedman J
TJ
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; D049109:Cell Proliferation / Q000187:drug effects; D002478:Cells, Cultured; D003474:Curcumin / Q000138:chemical synthesis* / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D042783:Endothelial Cells / Q000187:drug effects; D004730:Endothelium, Vascular / Q000166:cytology; D051379:Mice; D008810:Mice, Inbred C57BL; D013329:Structure-Activity Relationship
D020533:Angiogenesis Inhibitors; D000970:Antineoplastic Agents; D003474:Curcumin