Gallic acid is widely distributed in plants, fruits and food and has a range of  biological activities. Many of the foods containing gallic acid have been used for years as natural remedies, and were relied upon by various cultures for their medicinal properties. Studies have shows that gallic acid has anti-cancer properties against leukemia, certain prostate, colon and lung cancer cells. Gallic acid has been shown to prevent cellular mutations and to be toxic to cancer cells, while having no negative effect on healthy cells. Similarly, coumarin derivatives display broad spectrum of biological activity, among them in vitro antiproliferative activity against human neoplasms is notable. Therefore, the multistep synthesis of gallic acid derivatives with coumarin components was designed to obtain substances potentially inhibiting growth of cancer cells.

We report the synthesis and anticancer assay of eight new esters – derivatives of substituted 7-hydroxycoumarins and gallic acid:

          Compounds 1-4                                 Compounds 5-8

R₁= H, CH₃; R₂, R₃ = H, COCH₃

The esters 1-8 were assayed for antiproliferative activity against human leukemia HL-60 and prostate cancer DU-145 cell lines. The antiproliferative effects were estimated in terms of growth inhibition percentage. They were shown to be higher or comparable to the antiproliferative effect of gallic acid. No harmful effect was observed for NIH 3T3 mouse embryonic fibroblast cells.

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