146497-07-6Relevant academic research and scientific papers
Synthesis and biological evaluation of aromatic enones related to curcumin
Robinson, Thomas Philip,Hubbard IV, Richard B.,Ehlers, Tedman J.,Arbiser, Jack L.,Goldsmith, David J.,Bowen, J. Phillip
, p. 4007 - 4013 (2007/10/03)
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.
Design, synthesis, and biological evaluation of angiogenesis inhibitors: Aromatic enone and dienone analogues of curcumin
Robinson, Thomas Philip,Ehlers, Tedman,Hubbard IV, Richard B.,Bai, Xianhe,Arbiser, Jack L.,Goldsmith, David J.,Bowen, J. Phillip
, p. 115 - 117 (2007/10/03)
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.
