4-Hydroxy-3-methyl-6-phenylbenzofuran-2-carboxylic acid ethyl ester derivatives as potent anti-tumor agents.
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.
Hayakawa
Ichiro
I
Exploratory Chemistry Research Laboratories, Sankyo Co. Ltd, Shinagawa-ku, 140-8710, Tokyo, Japan.
Shioya
Rieko
R
Agatsuma
Toshinori
T
Furukawa
Hidehiko
H
Naruto
Shunji
S
Sugano
Yuichi
Y
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
D000970:Antineoplastic Agents; D001572:Benzofurans; D002264:Carboxylic Acids; D004952:Esters; C105430:benzofuran