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

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

研究成果: 雜誌貢獻文章同行評審

20 引文 斯高帕斯(Scopus)

摘要

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 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.
原文英語
頁(從 - 到)278-293
頁數16
期刊European Journal of Medicinal Chemistry
69
DOIs
出版狀態已發佈 - 2013
對外發佈

ASJC Scopus subject areas

  • 藥物發現
  • 有機化學
  • 藥理

指紋

深入研究「Structure-based design, synthesis and biological evaluation of novel anthra[1,2-d]imidazole-6,11-dione homologues as potential antitumor agents」主題。共同形成了獨特的指紋。

引用此