| abstract |
To search for novel anti-tumor drug candidates from 2-arylnaphthyridin-4-ones (ANs), we have designed and synthesized a series of 3'-hydroxy or 6-hydroxy derivatives of ANs. After screening for antitumor activity, it has been found that most of these compounds have significant activity. Among them, 2-(3-hydroxyphenyl)-5-methyl-1,8-naphthyridin-4(1H)-one (67) is the most promising. In the preliminary mechanism of action, treatment of Hep3B hepatoma cells with Compound 67 revealed that its mechanism of action was affected by microtubules and metastasis-related proteins. Then, the corresponding phosphate prodrug (86) of Compound 67 was tested against the anti-tumor activity of the Hep3B xenograft nude mouse model. |