| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1392896 | European Journal of Medicinal Chemistry | 2012 | 11 Pages |
Sixty-one curcumin-related compounds were synthesized and evaluated for their anticancer activity toward cultured prostate cancer PC-3 cells, pancreas cancer Panc-1 cells and colon cancer HT-29 cells. Inhibitory effects of these compounds on the growth of PC-3, Panc-1 and HT-29 cells were determined by the MTT assay. Compounds E10, F10, FN1 and FN2 exhibited exceptionally potent inhibitory effects on the growth of cultured PC-3, Panc-1 and HT-29 cells. The IC50 for these compounds was lower than 1 μM in all three cell lines. E10 was 72-, 46- and 117-fold more active than curcumin for inhibiting the growth of PC-3, Panc-1 and HT-29 cells, respectively. F10 was 69-, 34- and 72-fold more active than curcumin for inhibiting the growth of PC-3, Panc-1 and HT-29 cells, respectively. FN1 and FN2 had about the same inhibitory effect as E10 and F10 toward Panc-1 cells but were less active than E10 and F10 toward PC-3 and HT-29 cells. The active compounds were potent stimulators of apoptosis. The present study indicates that E10, F10, FN1 and FN2 may have useful anticancer activity.
Graphical abstractWe report here on the synthesis and inhibitory effects of 61 curcumin-related compounds on the growth of cultured human prostate, pancreas and colon cancer cells. E10, F10, FN1 and FN2 were many-fold more active than curcumin.Figure optionsDownload full-size imageDownload as PowerPoint slideHighlights► Curcumin has been widely studied as an inhibitor of carcinogenesis. ► Sixty-one curcumin-related compounds were tested for effects on growth of cultured cancer cells. ► Many curcumin-related compounds inhibited the growth of prostate, pancreas and colon cancer cells. ► The most active curcumin-related compound was 46- to 117-fold more active than curcumin. ► Active curcumin-related compounds stimulated apoptosis in prostate cancer cells.
