Synthesis and cytotoxicity of methyl-4,8-dihydrobenzo[1,2-b:5,4-b']dithiophene-4,8-dione derivatives. |
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| Authors: | Y H Chao S C Kuo K Ku I P Chiu C H Wu A Mauger H K Wang K H Lee |
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| Institution: | Division of Medicinal Chemistry and Natural Products, School of Pharmacy, University of North Carolina, Chapel Hill 27599-7360, USA. |
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| Abstract: | 2- and 3-Methyl-4,8-dihydrobenzo1,2-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-dihydrobenzo1,2-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). |
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