Abstract

A series of coumarins and related compounds were synthesized and screened as potential anti-tumor-promoting agents by examining the ability of the compound to inhibit Epstein-Barr virus early antigen (EBV-EA) activation induced by 12-O.-tetradecanoylphorbol-13-acetate (TPA) in Raji cells. The most promising compound in this in vitro. assay, 7,8-di(3-methyl-2-butenyloxy)coumarin (17), showed confirmed chemopreventive activity in an in vivo. two-stage assay of mouse skin tumors (DMBA/TPA). This investigation also confirmed an important role for the prenyl moiety, and, possibly, for the dimethylpyran substructure, on the anti-tumor-promoting activity.

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