title: Synthesis and cytotoxicity of methyl-4,8-dihydrobenzo[1,2-b:5,4-b']dithiophene-4,8-dione derivatives.
abstract: 2- and 3-Methyl-4,8-dihydrobenzo[1,2-b:5,4-b']dithiophene-4,8-dione and related derivatives were synthesized and evaluated in vitro by NCI against eight cancer types. Compounds 12-15 showed significant activity against melanoma, NCI-H23 non-small cell lung cancer, and MDA-MB-435 and MDA-N breast cancer cell lines; 2-hydroxymethyl-4,8-dihydrobenzo[1,2-b:5,4-b']dithiophene-4,8-dion e (13) showed the highest activity against melanoma (mean log GI50 = -7.74) and the highest overall potency (mean log GI50 = -6.99).
authors.affiliation: Division of Medicinal Chemistry and Natural Products, School of Pharmacy, University of North Carolina, Chapel Hill 27599-7360, USA.
authors.forename: Y H
authors.initials: YH
authors.lastname: Chao
authors.forename: S C
authors.initials: SC
authors.lastname: Kuo
authors.forename: K
authors.initials: K
authors.lastname: Ku
authors.forename: I P
authors.initials: IP
authors.lastname: Chiu
authors.forename: C H
authors.initials: CH
authors.lastname: Wu
authors.forename: A
authors.initials: A
authors.lastname: Mauger
authors.forename: H K
authors.initials: HK
authors.lastname: Wang
authors.forename: K H
authors.initials: KH
authors.lastname: Lee
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D013876:Thiophenes / Q000138:chemical synthesis* / Q000494:pharmacology; D014407:Tumor Cells, Cultured
chemical_list: C120943:2-hydroxymethyl-4,8-dihydrobenzo(1,2-b-5,4-b')dithiophene-48-dione; D000970:Antineoplastic Agents; D013876:Thiophenes