| Summary: | Seventeen new flavone derivatives substituted at the 4′-OH position were designed, synthesized and evaluated for their anticancer and antibacterial activities. Among them, compounds <b>3</b>, <b>4</b>, <b>6f</b>, <b>6e</b>, <b>6b</b>, <b>6c</b> and <b>6k</b> demonstrated the most potent antiproliferative activities against a human erythroleukemia cell line (HEL) and a prostate cancer cell line (PC3). The results also showed that the IC<sub>50</sub> value of compounds <b>3</b>, <b>4</b>, <b>6f</b>, <b>6e</b>, <b>6b</b>, <b>6c</b> and <b>6k</b> were close to that of the anticancer drug cisplatin (DDP) and lower than that of apigenin. All of the derivatives did not present antibacterial activities. The structure−activity relationships evaluation showed that the configuration of methyl amino acid might affect their biological activities.
|
|---|
