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Synthesis and anti-tumor activity of Fissitungfine B compounds.

Authors :
Zhou S
Zhou X
Huang G
Source :
Chemical biology & drug design [Chem Biol Drug Des] 2022 Sep; Vol. 100 (3), pp. 305-312. Date of Electronic Publication: 2022 Jul 05.
Publication Year :
2022

Abstract

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 <subscript>50</subscript>  = 3.82 ± 0.56 μM, MCF-7 was IC <subscript>50</subscript>  = 5.53 ± 0.68 μM, and A-549 was IC <subscript>50</subscript>  = 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.<br /> (© 2022 John Wiley & Sons Ltd.)

Details

Language :
English
ISSN :
1747-0285
Volume :
100
Issue :
3
Database :
MEDLINE
Journal :
Chemical biology & drug design
Publication Type :
Academic Journal
Accession number :
35763543
Full Text :
https://doi.org/10.1111/cbdd.14108