AI Article Synopsis
- A series of 2,7-diamidofluorenones were created and tested using SRB assay, revealing some compounds with strong antitumor properties in the submicromolar range.
- Ten compounds were highlighted in the NCI screening, with 3c showing the highest activity (GI50=1.66 μM).
- Compound 3c also inhibited topoisomerase I, suggesting that fluorenones could be promising candidates for future anticancer drug development.
Article 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.
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| http://dx.doi.org/10.1016/j.bmc.2013.09.006 | DOI Listing |
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