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化合物4g
Chemical Biology & Drug Design · 2022 ·Vol. 100 ·期 3 ·305-312 · IF 2.873

Synthesis and anti-tumor activity of Fissitungfine B compounds

Shiyang Zhou,Xiaofeng Zhou,Gangliang Huang

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.

研究领域: 药物化学 · 肿瘤学 · 合成化学
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