Synthesis and cytotoxicity of methyl-4,8-dihydrobenzo[1,2-b : 5,4-b ']dithiophene-4,8-dione derivatives

Authors
Chao, YH Kuo, SC Ku, K Chiu, IP Wu, CH Mauger, A Wang, HK Lee, KH
Citation
Yh. Chao et al., Synthesis and cytotoxicity of methyl-4,8-dihydrobenzo[1,2-b : 5,4-b ']dithiophene-4,8-dione derivatives, BIO MED CH, 7(6), 1999, pp. 1025-1031
Citations number
6
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY
ISSN journal
09680896 → ACNP
Volume
7
Issue
6
Year of publication
1999
Pages
1025 - 1031
Database
ISI
SICI code
0968-0896(199906)7:6<1025:SACOM:>2.0.ZU;2-0
Abstract
2- and 3-Methyl-4,8-dihydrobenzo[1,2-b:5,4-b']dithiophene-4,8-dione and rel ated derivatives were synthesized and evaluated in vitro by NCI against eig ht cancer types. Compounds 12-15 showed significant activity against melano ma, NCl-H23 non-small cell lung cancer, and MDA-MB-435 and MDA-N breast can cer cell lines; 2-hydroxymethyl-4,8-dihydrobenzo[1,2-b:5,4-b']dithiophene4, 8-dione (13) showed the highest activity against melanoma (mean log GI(50) = -7.74) and the highest overall potency (mean log GI50 = -6.99). (C) 1999 Published by Elsevier Science Ltd. All rights reserved.