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).
Synthesis and Cytotoxicity of Acetyl-4H, 9H-Naphto[2,3-b]thiophene-4,9-diones.-The preparation of new mono-and diacetyl-substituted derivatives of naphtho[2,3-b]thiophene-4,9-dione is described and their in vitro toxicity against various cancer cell types is evaluated. -(HUANG, L.-J.; KUO, S.-C.; PERNG, C.-Y.; CHAO, Y.-H.; WU, T.-S.; MCPHAIL, A. T.; MAUGER, A.; CHENG, H.-H.; LEE, K.-H.; Bioorg. Med.
Synthesis and Cytotoxicity of 2- Derivatives.-In vitro evaluation of title compounds (Ia) and (IIa) and their derivatives against eight cancer types shows that all compounds have significant activity. However, monosubstituted compounds, in general, display stronger selectivity than the corresponding disubstituted compounds. The derivatives (IIa) and, especially, (Ic) (possessing the highest overall potency) are candidates for further in vivo
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.