In order to explore the potential anti-tumor activity functional molecules, a series of Fissitungfine B derivatives were designed and synthesized. Their anti-tumor activity effects on Hela, MCF-7 and A-549 cell lines were evaluated in vitro. The results showed that some of these Fissitungfine B derivatives exhibited moderate to good anti-tumor activities. Especially, compound 4 g with the highest inhibitory activities against all tested cell lines with the Hela was IC 50 = 3.82 ± 0.56 μM, MCF-7 was IC 50 = 5.53 ± 0.68 μM, and A-549 was IC 50 = 4.55 ± 0.53 μM. Furthermore, the compounds 4 g have higher inhibitory effects on TDP2 in vitro . In vivo, the biological activities assay results showed that the target compound 4 g had a good inhibitory effect on tumor growth . The target compound 4 g could inhibit tumor growth well, which might be use as a candidate drug or lead compound for further research and development anti-tumor agents.
In this study, a series of novel 7 H -benzo [ c ] [1,3] dioxolo [4, 5- f ] chromen-7-one derivatives were obtained by structural modification of the lead compounds with Fissitungfine B. A total 15 compounds were designed, synthesized and evaluated as inhibitors of tumor. These target compounds have the novel chemical structures that named three six-membered rings including one lactone six-membered ring. In vitro assay, the results showed that the target compounds have a broad spectrum and strong of anti-tumor activity. Such as the target compound 4n to MCF-7 was IC 50 = 0.35 ± 0.01 μM, to A-549 was IC 50 = 0.37 ± 0.01 μM, to Hela was IC 50 = 0.56 ± 0.02 μM, to MDC-803 was IC 50 = 0.53 ± 0.02 μM and COLO-205 was IC 50 = 0.50 ± 0.02 μM in vitro . At the same time, in vivo anti-tumor activity assay results showed that the target compounds had a good inhibitory effect on tumor growth. Among them, the target compound 4n had the best anti-tumor activity, it could inhibit tumor growth well at a low dose. The target compound 4n could be used as a candidate drug for further research and development, in order to be used as early as application in the clinical treatment of tumors.
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