A5014591308- X-ray Diffraction in Crystallography
- Crystallization and Solubility Studies
- Metal complexes synthesis and properties
- Magnetism in coordination complexes
- Quinazolinone synthesis and applications
- Synthesis and Characterization of Heterocyclic Compounds
- Lanthanide and Transition Metal Complexes
- Crystal structures of chemical compounds
- Synthesis and Biological Evaluation
- Synthesis and Reactivity of Heterocycles
- Plant Virus Research Studies
- Ferrocene Chemistry and Applications
- Metal-Catalyzed Oxygenation Mechanisms
- Trace Elements in Health
- Natural product bioactivities and synthesis
- Plant-Microbe Interactions and Immunity
- Chemical Synthesis and Analysis
- Synthesis and biological activity
- Click Chemistry and Applications
- Bioactive Compounds and Antitumor Agents
- HIV/AIDS drug development and treatment
- Pharmacogenetics and Drug Metabolism
- Chemical synthesis and alkaloids
- Drug Transport and Resistance Mechanisms
- Plant biochemistry and biosynthesis
Palacký University Olomouc
2011-2024
Regional Centre of Advanced Technologies and Materials
2011-2024
Institute of Molecular and Translational Medicine
2014-2018
Czech Academy of Sciences, Institute of Experimental Botany
2002-2015
Howard Hughes Medical Institute
2005
Academy of Sciences of Moldova
1990
A series of eight N ‐heterocyclic carbenes (NHC) gold(I) complexes, involving 1,3‐bis(2,6‐diisopropylphenyl)imidazol‐2‐ylidene (iPr) ligand in combination with 6‐mercaptopurine derivatives (HL 1–8 ), has been prepared and thoroughly characterized, including elemental analysis, mass spectrometry, infrared multinuclear NMR spectroscopy, single crystal X‐ray analysis. The showing general composition [Au (iPr)(L n )] 1 – 8 , were evaluated for their vitro cytotoxicity against four human cancer...
One of several potential approaches to study mechanisms action biologically active compounds is develop their agonists and antagonists. In the present study, we report identification first known molecule antagonizing activity plant hormone cytokinin at receptor level. This compound, 6-(2-hydroxy-3-methylbenzylamino)purine, designated PI-55 in structurally closely related 6-benzylaminopurine, but substitutions specific positions aromatic side chain strongly diminished its conferred...
In this work, we describe synthesis of conjugates betulinic acid with substituted triazoles prepared via Huisgen 1,3-cycloaddition. All compounds contain free 28-COOH group. Allylic bromination protected by NBS gave corresponding 30-bromoderivatives, their substitution sodium azides produced 30-azidoderivatives and these were subjected to CuI catalysed 1,3-cycloaddition give the final conjugates. Reactions had moderate high yields. new tested for in vitro cytotoxic activities on eight cancer...
Herein we report the polymer-supported synthesis of 3,4-dihydro-2H-1,4-oxazine-3-carboxylic acid derivatives using immobilized Fmoc-Ser(tBu)-OH and Fmoc-Thr(tBu)-OH as starting materials. After solid-phase-synthesis N-alkyl-N-sulfonyl/acyl intermediates, target dihydrooxazines were obtained trifluoroacetic acid-mediated cleavage from resin. This approach was also studied for preparation dihydrothiazines Fmoc-Cys(Trt)-OH. Inclusion triethylsilane in cocktail resulted stereoselective formation...
The in vitro antitumour activity studies on a panel of human cancer cell lines (A549, HeLa, G-361, A2780, and A2780R) the combined vivo ex testing L1210 lymphocytic leukaemia model were performed cis-[PtCl2(naza)2] complexes (1–3) involving 7-azaindole derivatives (naza). platinum(II) showed significantly higher cytotoxic effects cell-based models, as compared with cisplatin, ability to avoid acquired resistance A2780R line cisplatin. (applied at same dose cisplatin) revealed their positive...
The platinum(II) oxalato complexes [Pt(ox)(naza)2] (1-3) were synthesized and characterized by elemental analysis (C, H, N), multinuclear NMR spectroscopy ((1)H, (13)C, (15)N, (195)Pt) electrospray ionization mass spectrometry (ESI-MS); naza = 4-chloro-7-azaindole (4Claza; 1), 3-bromo-7-azaindole (3Braza; 2) or 4-bromo-7-azaindole (4Braza; 3). prepared substances screened for their in vitro antitumor activity on the osteosarcoma (HOS) breast adenocarcinoma (MCF7) human cancer cell lines,...
Simple solid-phase synthesis of 3,10-dihydro-2H-benzo[e]imidazo[1,2-b][1,2,4]thiadiazin-2-one 5,5-dioxides is described, with Fmoc-α-amino acids and 2-nitrobenzenesulfonyl chlorides (2-NosCls) being the key building blocks. were immobilized on Wang resin transformed to corresponding 2-nitrobenzenesulfonamides in two steps. After reduction nitro group, Fmoc-thioureas synthesized followed by cyclization 1,2,4-benzothiadiazine-1,1-dioxide scaffold diisopropylcarbodiimide (DIC). Cleavage Fmoc...
Aim: From betulinic acid (1a), we synthesized 30-oxobetulinic (2a) that is highly cytotoxic against many cancer cell lines; however, its generic toxicity the main obstacle in further development as cytostatic. Methodology & results: 2a, prepared a new class of compounds – nonsymmetrical azines and tested their vitro cytotoxicity. All with free 28-COOH group (4a–4e) were selectively T-lymphoblastic leukemia line CCRF-CEM exhibited dose-dependent inhibition RNA DNA synthesis other cell-cycle...
Abstract Six platinum(II) complexes of the general formula [Pt(cbdc)(HL n ) 2 ] ( 1 – 6 ; cbdc = cyclobutane‐1,1‐dicarboxylate and HL –HL benzyl‐substituted 6‐benzylamino‐2‐chloro‐9‐isopropylpurine derivatives) have been synthesized by reaction [Pt(cbdc)(dmso) with corresponding compound. The prepared were characterized elemental analysis FTIR, Raman NMR H, 13 C, 15 N 195 Pt) spectroscopy. Based on results these techniques, it can be concluded that central Pt II atom is coordinated to two...
An efficient method is described for the solid-supported synthesis of imidazo[4,5-b]pyridines and imidazo[4,5-c]pyridines from 2,4-dichloro-3-nitropyridine. The key pyridine building block was reacted with polymer-supported amines, followed by replacement second chlorine nitro group reduction, imidazole ring closure aldehydes. Depending on combination solution-phase reagents, strategy allowed simple preparation target trisubstituted derivatives variable positioning nitrogen atom....