title: A library synthesis of 4-hydroxy-3-methyl-6-phenylbenzofuran-2-carboxylic acid ethyl ester derivatives as anti-tumor agents.
abstract: As a result of a hit-to-lead program using a technique of solution-phase parallel synthesis, a highly potent (2,4-dimethoxyphenyl)-[6-(3-fluorophenyl)-4-hydroxy-3-methylbenzofuran-2-yl]methanone (15b) was synthesized as an optimized derivative of 4-hydroxy-3-methyl-6-phenylbenzofuran-2-carboxylic acid ethyl ester (1), which was discovered as a screening hit from small-molecule libraries and exhibited selective cytotoxicity against a tumorigenic cell line.
authors.affiliation: Lead Discovery Research Laboratories, Sankyo Co. Ltd, Shinagawa-ku, Tokyo 140-8710, 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*; D001572:Benzofurans / Q000138:chemical synthesis*; D002264:Carboxylic Acids / Q000138:chemical synthesis*; D045744:Cell Line, Tumor; D020650:Combinatorial Chemistry Techniques / Q000379:methods; D006801:Humans
chemical_list: D000970:Antineoplastic Agents; D001572:Benzofurans; D002264:Carboxylic Acids