Design, synthesis, and anticancer activity evaluation of curcumol derivatives.

A new series of C-14 curcumol derivatives as potent anticancer agents were designed and synthesized by click reaction, whose structures were confirmed by 1H NMR,13C NMR, and HRMS analysis. All the synthesized compounds were evaluated for in vitro antitumor activity against colorectal cancer cell lines SW620 and HCT116. Most of them exhibited higher inhibitory activity than curcumol. Especially, compound 3j shows good inhibitory activity against SW620 with IC50 value of 8.10 ± 0.13 µM. The structure-activity relationships (SARs) of these derivatives were discussed. In addition, flow cytometry revealed that compound 3j induced SW620 cells apoptosis by facilitating apoptosis-related proteins expressions. Our findings suggested that fluorine functional group on phenyl ring tended to increase the anticancer activity.

Design, synthesis, and biological evaluation of C-8 modified curcumol derivatives against colorectal cancer cell lines.

A series of structurally modified curcumol derivatives at C-8 position were designed and synthesized, whose structures were confirmed by 1H NMR,13C NMR, and HRMS analysis. The tested compounds were evaluated for in vitro antitumor activity against colorectal cancer cell lines SW620, HCT116, and CaCo2. Many of the tested candidates exhibited higher inhibition efficiency than curcumol. Among them, compound 3 l shows the best inhibitory effect on the viability of SW620 with IC50 value of 19.90 ± 0.64 µM. The structure-activity relationships of these derivatives were discussed, which showed that the introduction of amino or aryl groups tended to increase the anti-cancer activity. In addition, compound 3 l may inhibit cancer cell proliferation through triggering cell apoptosis.