A5037975094- Fluorine in Organic Chemistry
- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Synthesis and Reactions of Organic Compounds
- Chemical Synthesis and Analysis
- Carbohydrate Chemistry and Synthesis
- Porphyrin and Phthalocyanine Chemistry
- Oxidative Organic Chemistry Reactions
- Analytical Chemistry and Chromatography
- Cyclopropane Reaction Mechanisms
- Peptidase Inhibition and Analysis
- Adenosine and Purinergic Signaling
- Epigenetics and DNA Methylation
- Photodynamic Therapy Research Studies
- RNA Interference and Gene Delivery
- Phase Equilibria and Thermodynamics
- Scientific Measurement and Uncertainty Evaluation
- Click Chemistry and Applications
- Bacillus and Francisella bacterial research
- Asymmetric Synthesis and Catalysis
- Organic Chemistry Cycloaddition Reactions
- Molecular Junctions and Nanostructures
- Radical Photochemical Reactions
- Bacterial Genetics and Biotechnology
- Molecular spectroscopy and chirality
Charles University
2022-2025
University of Chemistry and Technology, Prague
2000-2025
University of New York in Prague
2025
General University Hospital in Prague
2023
National Institute of Standards and Technology
2023
Université de Lorraine
2023
Czech Academy of Sciences, Institute of Organic Chemistry and Biochemistry
2010-2020
Czech Academy of Sciences
2014
National Institutes of Health
2007-2010
National Institute of Diabetes and Digestive and Kidney Diseases
2008-2010
Abstract INTRODUCTION: The molecular hybridization of three pharmacophores—benzothiazole, cyclobut-2-ene-1, 2-dione, and hydrazone—has led to the development novel compounds with diverse biological activities, including anticancer, anti-inflammatory, antiviral properties. Among these, certain derivatives demonstrated potent selective anticancer activity, particularly in CCRF-CEM HCT116 cell lines. Some also emitted green fluorescence, enabling organelle-specific imaging by fluorescence...
The protective antigen (PA) component of the anthrax toxin forms pores within low pH environment host endosomes through mechanisms that are poorly understood. It has been proposed pore formation is dependent on histidine protonation. In previous work, we biosynthetically incorporated 2-fluorohistidine (2-FHis), an isosteric analogue with a significantly reduced pK(a) ( approximately 1), into PA and showed pH-dependent conversion from soluble prepore to was unchanged. However, also observed...
Treatment of cleaned gold surfaces with dilute tetrahydrofuran or chloroform solutions tetraalkylstannanes (alkyl = methyl, ethyl, n-propyl, n-butyl) di-n-butylmethylstannyl tosylate under ambient conditions causes a self-limited growth disordered monolayers consisting alkyls and tin oxide. Extensive use deuterium labeling showed that the originate from stannane not impurities, trialkylstannyl groups are absent in monolayers, contrary to previous proposals. Methyl attached Sn atom...
Abstract 3‐Fluorofuran‐2(5 H )‐one ( 1 ) and three 3,4‐difluorofuran‐2(5 )‐ones 2 – 4 , α,β‐unsaturated lactones possessing fluorinated double bonds, were applied as dienophiles in Diels–Alder reactions with normal electron demand using diphenylisobenzofuran or cyclopentadiene dienes. In the same reactions, furan 2,3‐dimethylbuta‐1,3‐diene completely unreactive. Three structural factors of furan‐2(5 appeared to have an effect on reactivity, regioselectivity diastereoselectivity [4+2]...
Abstract Immune checkpoints regulate the immune system response. Recent studies suggest that flavonoids, known as phytoestrogens, may inhibit PD-1/PD-L1 axis. We explored potential of estrogens and 17 Selective Estrogen Receptor Modulators (SERMs) inhibiting ligands for checkpoint proteins (CTLA-4, PD-L1, PD-1, CD80). Our docking revealed strong binding energy values quinestrol, quercetin, bazedoxifene, indicating their to PD-1 CTLA-4. Quercetin modulate EGFR IL-6R alongside estrogen...
Abstract The binding of the Bacillus anthracis protective antigen (PA) to host cell receptor is first step toward formation anthrax toxin, a tripartite set proteins that include enzymatic moieties edema factor (EF), and lethal (LF). PA cleaved by furin‐like protease on surface followed donut‐shaped heptameric prepore. prepore undergoes major structural transition at acidic pH results in membrane spanning pore, an event which dictated interactions with necessary for entry EF LF into cell. We...
Multi‐orthogonal scaffolds can be useful for the attachment of several different compounds to same central skeleton. Such find applications in development protein mimics because their potential mimic distant epitopes structure. Three new tri‐orthogonal variants a previously reported scaffold have been developed that are suitable solid‐phase synthesis three peptides on Different chemical moieties were combined phased amino acids scaffolds: Fmoc‐ or Alloc‐protected amine, free TIPS‐protected...
Targeting of epigenetic mechanisms, such as the hydroxymethylation DNA, has been intensively studied, with respect to treatment many serious pathologies, including oncological disorders. Recent studies demonstrated that promising therapeutic strategies could potentially be based on inhibition TET1 protein (ten-eleven translocation methylcytosine dioxygenase 1) by specific iron chelators. Therefore, in present work, we prepared a series pyrrolopyrrole derivatives hydrazide (1) or hydrazone...
A series of metalloporphyrin dimers as Tröger's bases 1 or spiro-Tröger's 2 was prepared starting from five different C4-symmetry porphyrin derivatives substituted in meso-positions by Ph, 3-MeO-Ph, 4-MeO-Ph, 3,4-(MeO)2-Ph, 3,5-(MeO)2-Ph. Free-base porphyrins were converted to metalloporphyrins, which subsequently nitrated with nickel(II), copper(II), zinc(II) nitrate give β-nitrometalloporphyrins. These further reduced β-aminometalloporphyrins and treated a methanal equivalent under acidic...
Abstract Hydrofluoroethers (HFEs) represent a new family of promising engineering fluids suitable for technical cleaning and cooling electronic magnetic devices or as admixtures in refrigerant blends. Here, we report accurate data the liquid density at 0.1 MPa temperatures from $$273.15\,\text{K}$$ <mml:math xmlns:mml="http://www.w3.org/1998/Math/MathML"> <mml:mrow> <mml:mn>273.15</mml:mn> <mml:mspace /> <mml:mtext>K</mml:mtext> </mml:mrow> </mml:math> to $$343.15\,\text{K}$$...
Abstract A simple, sensitive and quick HPLC method was developed for the determination of ketoprofen in cell culture media (EMEM, DMEM, RPMI). Separation performed using a gradient on C18 column with mobile phase acetonitrile miliQ water acidified by 0.1 % (v/v) formic acid. The validated parameters including linearity, accuracy, precision, limit quantitation detection, as well robustness. response found linear over range 3–100 μg/mL demonstrated acquired value correlation coefficient...
Non‐natural compounds mimicking the actions of proteins and large peptides can find a plethora applications in modulating protein–protein interactions. In this study, biological properties three new tripodal trifunctional scaffolds designed for solid‐phase synthesis different on same scaffold were tested. Using model peptide sequences derived from receptor‐binding epitopes insulin or previously developed mimetics, quality scaffold‐derived probed as binders IGF‐1 receptors activators...
Pentamethinium indolium salts are promising fluorescence probes and anticancer agents with high mitochondrial selectivity. We synthesized two pentamethinium salts: a cyclic form quinoxaline directly incorporated in the chain (cPMS) an open substitution γ-position (oPMS). To better understand their properties, we studied interaction phospholipids (cardiolipin phosphatidylcholine) by spectroscopic methods (UV-Vis, fluorescence, NMR spectroscopy). Both compounds displayed significant affinity...