期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 21, 期 22, 页码 7125-7133出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2013.09.006
关键词
Tilorone; Fluorenones; Topoisomerase I; NCl 60-cell panel assay
资金
- Orient Europharma Co. Ltd., Taiwan
- Chi-Mei Medical Center [CMNDMC10210]
- National Science Council, Taiwan, R.O.C. [NSC 101-2113-M-016]
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 mu M) appeared to be the most active agent of this series. Furthermore, 3c attenuated topoisomerase I-mediated DNA relaxation at low micromolar concentrations. These results indicated that fluorenones have potential to be further developed into anticancer drugs. Crown Copyright (C) 2013 Published by Elsevier Ltd. All rights reserved.
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