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 (GI50 = 1.66 μM) 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.
Original language | English |
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Pages (from-to) | 7125-7133 |
Number of pages | 9 |
Journal | Bioorganic and Medicinal Chemistry |
Volume | 21 |
Issue number | 22 |
DOIs | |
Publication status | Published - Nov 15 2013 |
Externally published | Yes |
Keywords
- Fluorenones
- NCI 60-cell panel assay
- Tilorone
- Topoisomerase I
ASJC Scopus subject areas
- Drug Discovery
- Molecular Medicine
- Molecular Biology
- Biochemistry
- Clinical Biochemistry
- Pharmaceutical Science
- Organic Chemistry