A library synthesis of 4-hydroxy-3-methyl-6-phenylbenzofuran-2-carboxylic acid ethyl ester derivatives as anti-tumor agents.
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.
Hayakawa
Ichiro
I
Lead Discovery Research Laboratories, Sankyo Co. Ltd, Shinagawa-ku, Tokyo 140-8710, Japan.
Shioya
Rieko
R
Agatsuma
Toshinori
T
Furukawa
Hidehiko
H
Naruto
Shunji
S
Sugano
Yuichi
Y
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
D000970:Antineoplastic Agents; D001572:Benzofurans; D002264:Carboxylic Acids