Design, synthesis and antiproliferative evaluation of fluorenone analogs with DNA topoisomerase I inhibitory properties

…, DM Chang, KF Huang, CL Chen, TC Chen…

文献索引：Lee, Chia-Chung; Chang, Deh-Ming; Huang, Kuo-Feng; Chen, Chun-Liang; Chen, Tsung-Chih; Lo, Yang; Guh, Jih-Hwa; Huang, Hsu-Shan Bioorganic and Medicinal Chemistry, 2013 , vol. 21, # 22 p. 7125 - 7133

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被引用次数: 9

摘要

Abstract A series of 2, 7-diamidofluorenones were designed, synthesized, and screened by SRB assay. Some synthesized compounds exhibited antitumor activities in submicromolar range. Ten compounds (3a, 3b, 3c, 3g, 3j, 3l, 4a, 4h, 4i, and 4j) were also selected by NCI screening system and 3c (GI 50= 1.66 μM) appeared to be the most active agent of this series. Furthermore, 3c attenuated topoisomerase I-mediated DNA relaxation at low ...