title: 4-Hydroxy-3-methyl-6-phenylbenzofuran-2-carboxylic acid ethyl ester derivatives as potent anti-tumor agents.
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.
authors.affiliation: Exploratory Chemistry Research Laboratories, Sankyo Co. Ltd, Shinagawa-ku, 140-8710, Tokyo, Japan.
authors.forename: Ichiro
authors.initials: I
authors.lastname: Hayakawa
authors.forename: Rieko
authors.initials: R
authors.lastname: Shioya
authors.forename: Toshinori
authors.initials: T
authors.lastname: Agatsuma
authors.forename: Hidehiko
authors.initials: H
authors.lastname: Furukawa
authors.forename: Shunji
authors.initials: S
authors.lastname: Naruto
authors.forename: Yuichi
authors.initials: Y
authors.lastname: Sugano
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001572:Benzofurans / Q000138:chemical synthesis* / Q000494:pharmacology; D002264:Carboxylic Acids / Q000138:chemical synthesis* / Q000494:pharmacology; D045744:Cell Line, Tumor; D004952:Esters; D006801:Humans
chemical_list: D000970:Antineoplastic Agents; D001572:Benzofurans; D002264:Carboxylic Acids; D004952:Esters; C105430:benzofuran