Title 3,3′-((3-hydroxyphenyl)azanediyl)dipropionic acid derivatives as a promising scaffold against drug-resistant pathogens and chemotherapy-resistant cancer
Authors Kavaliauskas, Povilas ; Acevedo, Waldo ; Mickevičiūtė, Eglė ; Grigalevičiūtė, Ramunė ; Grybaitė, Birutė ; Sapijanskaitė-Banevič, Birutė ; Pranaitytė, Guoda ; Petraitis, Vidmantas ; Petraitienė, Rūta ; Mickevičius, Vytautas
DOI 10.3390/pathogens14050484
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Is Part of Pathogens.. Basel : MDPI. 2025, vol. 14, iss. 5, art. no. 484, p. 1-27.. ISSN 2076-0817
Keywords [eng] 3,3′-((3-hydroxyphenyl)azanediyl)dipropionic acid ; β-amino acids derivatives ; antimicrobial activity ; multidrug-resistant pathogens ; head and neck cancer ; c-MET ; HER2
Abstract [eng] The synthesis and antimicrobial and anticancer activity of 3,3′-((3-hydroxyphenyl)azanediyl)dipropionic acid derivatives (2–25) against drug-resistant bacterial pathogens and FaDu head and neck cancer cells were investigated. The derivatives were synthesized through various methods, including esterification, hydrazinolysis, and condensation reactions. The compounds demonstrated structure-dependent antimicrobial activity, predominantly targeting Gram-positive pathogens. Compounds containing 4-nitrophenyl, 1-naphthyl, and 5-nitro-2-thienyl groups exhibited enhanced activity against S. aureus and E. faecalis. Additionally, compounds 5, 6, and 25 showed antiproliferative activity in cisplatin-resistant FaDu cells at low micromolar concentrations. The in silico modeling revealed that compound 25 interacts with the HER-2 and c-MET proteins. These compounds also induced significant oxidative stress in FaDu cells and demonstrated low cytotoxic activity in non-cancerous HEK293 cells. These results highlight the potential of N-aryl-substituted β-amino acid derivatives as promising scaffolds for the further development of novel amino acid-based antimicrobial and anticancer agents targeting drug-resistant pathogens and cancers.
Published Basel : MDPI
Type Journal article
Language English
Publication date 2025
CC license CC license description