Synthesis and evaluation of 3-methyl-4-oxo-6-phenyl-4,5,6,7-tetrahydrobenzofuran-2-carboxylic acid ethyl ester derivatives as potent antitumor agents.
For the construction of new combinatorial libraries, a lead compound was created by replacing the core structure of a hit compound discovered by screening for cytotoxic agents against a tumorigenic cell line. The newly designed compound maintained biological activity and allowed alternative library construction for antitumor drugs.
Hayakawa
Ichiro
I
Lead Discovery Research Laboratories, Sankyo Co., Ltd., Shinagawa-ku, Tokyo 140-8710, Japan. hayaka@sankyo.co.jp
Shioya
Rieko
R
Agatsuma
Toshinori
T
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; D004353:Drug Evaluation, Preclinical / Q000379:methods; D004952:Esters; D006801:Humans
D000970:Antineoplastic Agents; D001572:Benzofurans; D002264:Carboxylic Acids; D004952:Esters