Synthesis and anticancer activity of 7-hydroxycoumarinyl gallates.

Background: The search for anti-cancer agents includes naturally occurring substances and theirs modifications. Therefore we invented and designed compounds that represent fused derivatives of gallic acid with coumarins.

Methods: As a result, a series of 8 novel esters of gallic acid and 7-hydroxycoumarins were synthesized and evaluated for anticancer activity. The structures of the compounds were established by IR, (1)H, (13)C NMR and HR MS spectra. The esters were assayed for antiproliferative activity against human leukemia HL-60 and prostate cancer DU145 cell lines. The activity of novel esters was evaluated by cell viability assays as well as by analysis of cell cycle and cell death mechanism.

Results: The esters were found to be of similar or higher activity than gallic acid. No pronounced harmful effect was observed in non-cancer cells.

Conclusions: The novel compounds represent an excellent starting point for the further optimization and the design of therapeutically effective anti-cancerous drugs.