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4-Hydroxy-3-methyl-6-phenylbenzofuran-2-carboxylic acid ethyl ester derivatives as potent anti-tumor agents
Authors:Hayakawa Ichiro  Shioya Rieko  Agatsuma Toshinori  Furukawa Hidehiko  Naruto Shunji  Sugano Yuichi
Institution:Exploratory Chemistry Research Laboratories, Sankyo Co. Ltd, Shinagawa-ku, 140-8710, Tokyo, Japan.
Abstract:Based on the structure of 4-hydroxy-3-methyl-6-phenylbenzofuran-2-carboxylic acid ethyl ester (1), which exhibits selective cytotoxicity against a tumorigenic cell line, (2,4-dimethoxyphenyl)-(4-hydroxy-3-methyl-6-phenylbenzofuran-2-yl)-methanone (18m) was designed and synthesized as a biologically stable derivative containing no ester group. Although the potency of 18m was almost the same as our initial hit compound 1, 18m is expected to last longer in the human body as an anticancer agent.
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