Background: Compounds featuring furan nucleus exhibit diverse biological properties. Lots of furan
derivatives have been explored as pharmaceutical compounds. Hence it is of great interest to explore furan derivatives
and their precursors as antitumor agents.
Objective: A series of novel furan derivatives and their precursors (1-36) were synthesized from α-haloketones
and β-dicarbonyl compounds.
Methods: The reactions between β-dicarbonyl compounds and α-haloketones under basic conditions produced
tricarbonyls or dihydrofurans, which were then condensed into their corresponding furan products. Their
potential antiproliferative activity in vitro against two human tumor cell lines-cervical (HeLa) and colorectal
(SW620) was evaluated using CCK-8 assay. Compounds 1 and 24 were selected for Western blot analysis.
Results: Pronounced anti-proliferative effect in the micromolar level was observed for compounds (1, 4, 17, 20,
21, 24, 27, 31 and 32) in HeLa cells, with their IC50 values ranging from 0.08 to 8.79μM. Additionally, furan
compounds (24, 26, 32 and 35) had moderate to potent anti-proliferative activity against the SW620 cell line.
Furthermore, the possible targets of these compounds were explored by Western blot analysis. The results indicated
that the candidates (compounds 1 and 24) exhibited excellent antiproliferative activity, which may be
mediated by promoting the activity of PTEN to suppress PI3K/Akt and Wnt/β-catenin signaling.
Conclusion: Most of the furan derivatives and their precursors reported herein exhibited moderate to excellent
anti-proliferative activity against HeLa cell line and/or SW620 cell line. Compounds 1 and 24, as well as their
analogues may be developed as promising anti-cancer agents.