Synthesis and anti-tumor activity of Fissitungfine B compounds

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 IC₅₀  = 3.82 ± 0.56 μM, MCF-7 was IC₅₀  = 5.53 ± 0.68 μM, and A-549 was IC₅₀  = 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.