Wydział Chemii

Marcin Stolarczyk

Aleksandra Wolska

Aleksandra Mikołajczyk

Iwona Bryndal

Jerzy Cieplik

Tadeusz Lis

Agnieszka Matera-Witkiewicz

2021

Molecules

26

2296/1-2296/23

10.3390/molecules26082296

Naukowa

Angielski

Artykuł

Enterococcus faecalis is known as a significant nosocomial pathogen due to its natural resistance to many antibacterial drugs. Moreover, it was found that E. faecalis infection causes inflammation, production of reactive oxygen species, and DNA damage to human gastric cancer cells, which can induce cancer. In this study, we synthesized and tested the biological activity of a new Schiff base, 5-[(4-ethoxyphenyl)imino]methyl-N-(4-fluorophenyl)-6-methyl-2-phenylpyrimidin-4-amine (3), and compared its properties with an analogous amine (2). In the biological investigation, 3 was found to have antibacterial activity against E. faecalis 29212 and far better anticancer properties, especially against gastric adenocarcinoma (human Caucasian gastric adenocarcinoma), than 2. In addition, both derivatives were non-toxic to normal cells. It is worth mentioning that 3 could potentially inhibit cancer cell growth by inducing cell apoptosis. The results suggest that the presence of the –C=N– bond in the molecule of 3 increases its activity, indicating that 5-iminomethylpyrimidine could be a potent core for further drug discovery research.

antibacterial activity, anticancer activity, apoptosis, pyrimidines, Schiff bases

CC-BY

http://dx.doi.org/10.3390/molecules26082296

http://www.mdpi.com/journal/metals