A5006189027- Cancer therapeutics and mechanisms
- Synthesis and Biological Evaluation
- Synthesis and biological activity
- Computational Drug Discovery Methods
- Cholinesterase and Neurodegenerative Diseases
- Bioactive Compounds and Antitumor Agents
- DNA and Nucleic Acid Chemistry
- Chemical synthesis and alkaloids
- Education, Psychology, and Social Research
- Structural and Chemical Analysis of Organic and Inorganic Compounds
- Photodynamic Therapy Research Studies
- Pesticide Exposure and Toxicity
- Nanoplatforms for cancer theranostics
- Synthesis and Reactivity of Sulfur-Containing Compounds
- Porphyrin and Phthalocyanine Chemistry
- RNA Interference and Gene Delivery
- Synthesis and Characterization of Heterocyclic Compounds
- Synthesis of heterocyclic compounds
- Advanced biosensing and bioanalysis techniques
- Click Chemistry and Applications
- Lexicography and Language Studies
- Linguistics, Language Diversity, and Identity
- Linguistic research and analysis
- Synthetic Organic Chemistry Methods
- Discourse Analysis and Cultural Communication
University of Pavol Jozef Šafárik
2012-2024
Institute of Chemistry of the Slovak Academy of Sciences
2008-2021
A series of novel tacrine derivatives and tacrine-coumarin heterodimers were designed, synthesized, biologically evaluated for their potential inhibitory effect on both acetylcholinesterase (AChE) butyrylcholinesterase (BuChE). Of these compounds, heterodimer 7c derivative 6b found to be the most potent inhibitors human AChE (hAChE), demonstrating IC50 values 0.0154 0.0263 μM. Ligands 6b, 6c, exhibited highest levels activity against BuChE (hBuChE), that range from 0.228 0.328 Docking...
Five novel proflavine−dithiazolidinone derivatives 4a−4e have been designed and synthesized by the reaction of dialkyl acridin-3,6-diyl dithioureas 3a−3e with methyl bromoacetate. The binding affinity dithiazolidinone hydrochlorides 5a−5e calf thymus DNA plasmid (pUC19) was investigated a variety spectroscopic techniques including UV−vis, fluorescence, CD spectroscopy. effects on thermal denaturation profiles were also studied. From spectrophotometric spectrofluorimetric titrations,...
The reaction between N-(anthracen-9-yl)-N′-ethylthiourea (1) and methyl bromoacetate yielded mainly 2-[(anthracen-9-yl)imino]-3-ethyl-1,3-thiazolidin-4-one (2), together with some of the regioisomeric 3-(anthracen-9-yl)-2-ethylimino-1,3-thiazolidin-4-one (3). structures products were elucidated by NMR techniques and, for 3, X-ray crystallographic analysis. Treatment 1 bromoacetyl bromide again 2 but a reversed product distribution ratio, thus providing an interesting unexpected...
The design of new heterodimeric dual binding site acetylcholinesterase inhibitors constitutes the main goal-directed to development anticholinesterase agents with expanded pharmacological profile. Multi-target compounds are usually designed by combining in a hybrid molecule two or more pharmacophoric moieties that known enable interaction selected molecular targets.All were tested for their inhibitory activity on human AChE/BChE. Ellman´s method was used determine inhibition kinetics and...
The involvement of G-quadruplex (G4) structures in nucleic acids various molecular processes cells such as replication, gene-pausing, the expression crucial cancer-related genes and DNA damage repair is well known. compounds targeting G4 usually bind directly to structure, but some ligands can also facilitate folding unfolded G-rich sequences stabilize them even without presence monovalent ions sodium or potassium. Interestingly, G4-ligand complexes show a clear induced CD signal, feature...
Abstract The regioselective syntheses of 3‐alkyl(aryl)‐2‐(anthracen‐9′‐ylimino)‐1,3‐thiazolidin‐4‐ones (2) and 2‐alkyl(aryl)imino‐3‐(anthracen‐9′‐yl)‐1,3‐thiazolidin‐4‐ones (3) from N ‐(anthracen‐9‐yl)‐ ′‐alkyl(aryl)thioureas were accomplished effectively using methyl bromoacetate bromoacetyl bromide, respectively. Detailed structural characteristics confirmed mainly by NMR techniques. mass spectrometric behavior the resulting sets compounds known structures was shown to be characteristic...
The authors report on the synthesis and biological evaluation of new compounds whose structure combines tacrine indole moieties. Tacrine-indole heterodimers were designed to inhibit cholinesterases β-amyloid formation, cross blood-brain barrier. most potent acetylcholinesterase inhibitors 3c 4d (IC50 = 25 39 nM, respectively). Compound displayed considerably higher selectivity for relative human plasma butyrylcholinesterase in comparison compound (selectivity index: IC50...
A series of novel 3,9-disubstituted acridines were synthesized and their biological potential was investigated. The synthetic plan consists eight reaction steps, which produce the final products, derivatives 17a–17j, in a moderate yield. principles cheminformatics computational chemistry applied order to study relationship between physicochemical properties activity at cellular molecular level. selected acridine studied presence DNA using spectroscopic (UV-Vis, circular dichroism, thermal...
The synthesis, structure and reactivity of 9-isothiocyanatoanthracene ( 5 ) likewise the conformation corresponding thioureas 6a - 6i have been studied. 13 C NMR substituent chemical shift values NCS group correlations between spectral parameters (IR, NMR) rate constans reactions , acridin-9-yl 14 ), phenyl 15 benzoyl isothiocyanate 16 with butylamine were found. Significant increase fluorescence synthesized anthracenylthioureas amino acid rests refers to possibility use as potential biomarker.