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A series of structurally modified curcumol derivatives at C-8 position were designed and synthesized, whose structures were confirmed by  1 H NMR, 13 C 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 IC 50  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.

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