Abstract
Seventeen new flavone derivatives substituted at the 4′-OH position were designed, synthesized and evaluated for their anticancer and antibacterial activities. Among them, compounds 3, 4, 6f, 6e, 6b, 6c and 6k 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 IC50 value of compounds 3, 4, 6f, 6e, 6b, 6c and 6k 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.
Highlights
Cancer is ranked as the main cause of human death and the most important barrier to increasing life expectancy around the world
We found the activity of 6f was better than that of 6g, while 6b and 6c (D and L configuration, respectively) had similar IC50 values. These results indicate that the configuration of the methyl amino acid may have an effect on the biological activities
Seventeen new flavone derivatives were synthesized via N-amination in the 40 -position
Summary
Cancer is ranked as the main cause of human death and the most important barrier to increasing life expectancy around the world. There were 18.1 million new cases and 9.6 million cancer deaths worldwide in 2018 [1]. The need for developing new anticancer agents is growing [2]. Phytochemicals have become an important part of anticancer drugs. Over 75% of nonbiological anticancer drugs approved are either natural products or developed based on them [3]. Flavonoids, which are polyphenolic secondary metabolites mainly from plants and fungi, have diverse biological activities—especially anticancer activity through the regulation of different targets. Flavone was chosen as the lead skeleton for further structural modification for discovering new anticancer drug candidates
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