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ID: ALA1131509

Journal: J Med Chem

Title: Synthesis and cytotoxicity of 2-acetyl-4,8-dihydrobenzodithiophene-4, 8-dione derivatives.

Authors: Chao YH, Kuo SC, Wu CH, Lee CY, Mauger A, Sun IC, Morris-Natschke SL, Lee KH.

Abstract: 2-Acetyl-4,8-dihydrobenzo[1,2-b:4,5-b']dithiophene-4,8-dione (9) and 2-acetyl-4,8-dihydrobenzo[1,2-b:5,4-b']dithiophene-4,8-dione (19), together with 10 related mono- and disubstituted derivatives, were synthesized and evaluated in vitro by NCI against eight cancer types. All compounds showed significant activity against melanoma, HL-60 leukemia, NCI-H23 non-small-cell lung cancer, OVCAR-3 ovarian cancer, and MDA-MB-435 and MDA-N breast cancer cell lines. Compound 11, 2-(1'-acetoxyethyl)-4,8-dihydrobenzo[1,2-b:4,5-b']dithiophene-4, 8-dione, showed the highest overall potency (mean GI50 = 40 nM).

CiteXplore: 9804705

DOI: 10.1021/jm980394t