Synthesis and biological evaluation of aromatic enones and dienones related to curcumin
Hubbard, Richard Buell
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Curcumin, a natural product isolated from the spice turmeric, has been shown to exhibit a wide range of pharmacological activities including certain anticancer 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 antiangiogenic analog design, a series of structurally related compounds utilizing a substituted enone and dienone 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 straight forward synthetic preparation, these low molecular weight compounds are attractive leads for developing future angiogenic inhibitors.