Synthesis of novel sulphamethoxazole derivatives and exploration of their anticancer and antimicrobial properties.
Rita VaickelionienėVilma PetrikaitėIrena VaškevičienėAlvydas PavilonisVytautas MickevičiusPublished in: PloS one (2023)
A series of new derivatives based on sulfamethoxazole were designed and synthesized in this study. The structures of the new compounds were confirmed based on a comprehensive characterization of spectral data by applied IR and 1H as well as 13C NMR spectroscopy. The prepared compounds were tested for their anticancer and antimicrobial properties. Hydrazone 16b demonstrated convincing anticancer effect against all tested cell cultures such as human prostate carcinoma PPC-1 and human kidney carcinoma CaKi-1 cell lines, and human fibroblasts HF, n = 3. The most promising compound 16b showed higher activity against CaKi-1 cell line than the anticancer drugs axitinib and pazopanib used to treat renal cancer. Also, it was more active in the PPC-1 cell line compared to the approved PARP inhibitor Olaparib. Hydrazone 16b was also found to possess good antimicrobial properties against gram-positive bacteria strains of Staphylococcus aureus, Staphylococcus epidermidis, as well as Bacillus cereus.
Keyphrases
- staphylococcus aureus
- endothelial cells
- induced pluripotent stem cells
- biofilm formation
- prostate cancer
- pluripotent stem cells
- dna damage
- escherichia coli
- magnetic resonance imaging
- oxidative stress
- single cell
- heart failure
- electronic health record
- gram negative
- magnetic resonance
- squamous cell carcinoma
- bone marrow
- dna repair
- papillary thyroid
- optical coherence tomography
- multidrug resistant
- mesenchymal stem cells
- computed tomography
- wastewater treatment
- pseudomonas aeruginosa
- artificial intelligence
- bacillus subtilis
- oxide nanoparticles