Graduate Institute of Life Sciences, National Defense Medical Center, Taipei 114, Taiwan; School of Pharmacy, National Defense Medical Center, Taipei 114, Taiwan.
Bioorg Med Chem. 2013 Nov 15;21(22):7125-33. doi: 10.1016/j.bmc.2013.09.006. Epub 2013 Sep 13.
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.
设计、合成了一系列 2,7-二脒基芴酮，并通过 SRB 法进行了筛选。部分合成化合物在亚微摩尔浓度范围内表现出抗肿瘤活性。十种化合物（3a、3b、3c、3g、3j、3l、4a、4h、4i 和 4j）也通过 NCI 筛选系统进行了选择，其中 3c（GI50=1.66 μM）似乎是该系列中最活跃的化合物。此外，3c 在低微摩尔浓度下可抑制拓扑异构酶 I 介导的 DNA 松弛。这些结果表明芴酮类化合物具有进一步开发为抗癌药物的潜力。
