title: Thienopyridine and benzofuran derivatives as potent anti-tumor agents possessing different structure-activity relationships.
abstract: (3-Amino-6-thiophen-2-yl-thieno[2,3-b]pyridin-2-yl)phenylmethanone (3) was discovered as a new type of cytotoxic agent selective against a tumorigenic cell line. The molecular structure of a previously reported compound, (4-hydroxy-3-methyl-6-phenylbenzofuran-2-yl)phenylmethanone (2), had remarkably similar bioisosteric substructures to that of compound 3. Although the relationship between the molecular structure and biological activity of each derivative synthesized from these two hit compounds (2 and 3) were studied, unexpectedly no correlation was observed. However, after further synthetic study from 3, one of the most potent derivative (10k) having a different SAR profile from 2, was discovered.
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: Yuichi
authors.initials: Y
authors.lastname: Sugano
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001572:Benzofurans / Q000138:chemical synthesis* / Q000494:pharmacology; D045744:Cell Line, Tumor; D006801:Humans; D020128:Inhibitory Concentration 50; D011725:Pyridines / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D001572:Benzofurans; D011725:Pyridines; C446540:thienopyridine