Synthesis of fusidane triterpenoid Mannich bases as potential antibacterial and antitumor agents.
Elena V SalimovaLyudmila V ParfenovaDiana V IshmetovaLiana F ZainullinaYulia V VakhitovaPublished in: Natural product research (2023)
Mannich bases (8 examples) were synthesized via aminomethylation of fusidane propargyl esters. In vitro antimicrobial screening against key ESKAPE pathogens showed that the fusidic acid based Mannich products exhibit a high antimicrobial effect against Gram-positive bacteria Staphylococcus aureus and the fungus Cryptococcus neoformans . Moreover, the cytotoxic effect of fusidic acid and its analogs, which showed high antibacterial activity, was determined by MTT assay on cancer HepG2, HCT-116, SH-SY5Y, MCF-7, A549 and conditionally normal cells HEK293. A remarkable cytotoxic activity of fusidic acid propargyl ester and its aminomethylene derivatives against cancer and nontumoral HEK293 cells with IC 50 values within 4.2-25 µM was found.
Keyphrases
- staphylococcus aureus
- cell cycle arrest
- induced apoptosis
- papillary thyroid
- squamous cell
- gram negative
- endoplasmic reticulum stress
- pi k akt
- oxidative stress
- silver nanoparticles
- squamous cell carcinoma
- breast cancer cells
- lymph node metastasis
- biofilm formation
- cell proliferation
- antimicrobial resistance
- pseudomonas aeruginosa
- candida albicans
- human health
- structure activity relationship