Structure-based design, synthesis and biological evaluation of novel anthra[1,2-d]imidazole-6,11-dione homologues as potential antitumor agents

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• 作者：Tsung-Chih Chen ; Dah-Shyong Yu ; Kuo-Feng Huang ; Yung-Chien Fu ; Chia-Chung Lee ; Chun-Liang Chen ; Fong-Chun Huang ; Hsi-Hsien Hsieh ; Jing-Jer Lin ; Hsu-Shan Huang
• 关键词：Anthra[1 ; 2-d]imidazole-6 ; 11-dione ; Selectivity ratio ; NCI 60-cell panel assay ; Cytostatic and cytotoxic activities
• 刊名：European Journal of Medicinal Chemistry
• 出版年：November, 2013
• 年：2013
• 卷：69
• 期：Complete
• 页码：278-293
• 全文大小：2159 K

文摘

By using fragment-based design strategies, a series of 2-thio-substituted anthra[1,2-d]imidazole-6,11-diones were synthesized and evaluated for hTERT repressing activities, cell proliferations, and NCI 60-cell panel assay. Compounds Font">2, 3, 4, 11, 15 and 35 were selected by the NCI and 3, 4, 11 and 15 represent the GI₅₀, TGI and LC₅₀, respectively. Among them, all were moderate selectivity toward leukemia cancer except for 4 exhibited distinctive selectivity of CNS and renal cancer with 7.403 and 6.475. The overall of test compounds exhibited different cytostatic and cytotoxic activities for further developing potential application as anticancer drugs.