A5000273439- X-ray Diffraction in Crystallography
- Crystallization and Solubility Studies
- Synthesis and Characterization of Heterocyclic Compounds
- Synthesis and Biological Evaluation
- Synthesis and biological activity
- Axial and Atropisomeric Chirality Synthesis
- Synthesis and Reactions of Organic Compounds
- Molecular spectroscopy and chirality
- Catalytic Cross-Coupling Reactions
- Cancer-related Molecular Pathways
- Analytical Chemistry and Chromatography
- Sulfur-Based Synthesis Techniques
- Catalytic C–H Functionalization Methods
- Chemical Reaction Mechanisms
- Chemical Synthesis and Analysis
- Electrochemical Analysis and Applications
- Chemical synthesis and alkaloids
- Cancer Mechanisms and Therapy
- Multicomponent Synthesis of Heterocycles
- Advanced Breast Cancer Therapies
- Synthesis and Biological Activity
- Alkaloids: synthesis and pharmacology
- Fluorine in Organic Chemistry
- Carbohydrate Chemistry and Synthesis
- Molecular Sensors and Ion Detection
Palacký University Olomouc
2016-2025
Institute of Molecular and Translational Medicine
2013
Cyclacel Pharmaceuticals (United Kingdom)
2006
Brock University
2004-2006
Czech Academy of Sciences, Institute of Experimental Botany
2006
In a routine screening of our small-molecule compound collection we recently identified 4-arylazo-3,5-diamino-1H-pyrazoles as novel group ATP antagonists with moderate potency against CDK2-cyclin E. A preliminary SAR study based on 35 analogues suggests ways in which the pharmacophore could be further optimized, for example, via substitutions 4-aryl ring. Enzyme kinetics studies lead and X-ray crystallography an inhibitor−CDK2 complex demonstrated that its mode inhibition is competitive....
New screen-printed sensor with a boron-doped diamond working electrode (SP/BDDE) was fabricated using large-area linear antenna microwave chemical deposition vapor system (LA-MWCVD) novel precursor composition. It combines the advantages of disposable printed sensors, such as tailored design, low cost, and easy mass production, excellent electrochemical properties BDDE, including wide available potential window, background currents, resistance, resistance to passivation. The newly prepared...
The synthesis of axially chiral benzimidazoles with a peri-substituted naphthalene and dimethylamino group at positions 1 2, respectively, was developed. We evaluated these compounds in the desymmetrization reaction...
The efficient Suzuki–Miyaura cross-coupling reaction of halogenated aminopyrazoles and their amides or ureas with a range aryl, heteroaryl, styryl boronic acids esters has been developed. method allowed incorporation problematic substrates: bearing protected unprotected pyrazole NH, as well the free amino N-amide group. Direct comparison chloro, bromo, iodopyrazoles in revealed that Br Cl derivatives were superior to iodopyrazoles, result reduced propensity dehalogenation. Moreover,...
Racemic 2-(2-trifluoromethyl)-1
Abstract Electrochemical oxidation of azoxystrobin, a systemic fungicide commonly used in agriculture to protect wide variety crops, was investigated using cyclic voltammetry with boron‐doped diamond electrode (BDDE) aqueous buffer solutions. Two pH independent irreversible anodic current peaks controlled mostly by diffusion were observed range (2 12) at potentials +1600 mV and +2150 vs. saturated silver‐silver chloride electrode. Mechanism the electrochemical proposed supported high...
A general and efficient synthesis of 4-substituted-1<italic>H</italic>-pyrazole-3,5-diamines was developed to access derivatives with an aryl, heteroaryl, or styryl group, which are otherwise relatively difficult prepare.
Inhibitors of cyclin-dependent kinases 9 have been developed as potential anticancer drugs for the treatment multiple myeloma. We previously prepared a library arylazo-3,5-diaminopyrazole inhibitors CDKs. Here, we describe novel member, AAP1742 (CDK9 inhibition with IC(50) = 0.28 μm), that reduces viability myeloma cell lines in low micromolar concentrations. Consistent CDK9, decreases phosphorylation RNA polymerase II and inhibits mRNA synthesis anti-apoptotic proteins Mcl-1, Bcl-2, XIAP,...
Abstract Halogenated aminopyrazoles have rarely been utilized in metal‐catalysed cross‐coupling reactions mainly due to the complexation of metal center, which deactivates catalyst. In this paper we reveal that appropriate combination palladium source and ligand enables efficient Suzuki–Miyaura with even challenging substrates such as halogenated aminopyrazoles. The Pd(OAc) 2 XPhos allowed coupling N ‐acetylaminopyrazoles, whereas Pd G2 was needed when unprotected were used. Generally,...
Prototropic tautomerism was used as a tool for the reductive dehalogenation of (hetero)aryl bromides and iodides, or dehalogenative sulfonation chlorides fluorides, using sodium sulfite sole reagent in an aqueous medium.
The electrochemical behavior of tolterodine, an antimuscarinic drug used to treat urge incontinence and overactive bladder, was investigated using cyclic differential pulse voltammetry at glassy carbon electrode. Electrooxidation tolterodine proceeds as a complex two-step pH-dependent process. Controlled potential electrolysis solutions performed platinum gauze electrode in methanolic, aqueous-methanolic acetonitrile media. Electrolyzed were analyzed liquid chromatography with electrospray...
The cyclization of 3-bromo-6-methoxy-2-(naphtho[2,3d][1,3]dioxol-5-ylaminomethyl)phenol (2) using tributyltinhydride under radical-mediated conditions was accompanied by spontaneous oxidation and 4) isolated as a side product.Isodecarine also prepared the catalytic debenzylation 7-benzyloxy-8-methoxy-2,3-methylendioxybenzo-[c]phenanthridine (5).This compound efficiently converted to 7benzyloxy-8-methoxy-5-methyl-2,3-methylenedioxybenzo[c]phenanthridinium trifluoromethanesulfonate (6) in high...
Axially chiral trifluoromethylbenzimidazolylbenzoic acid (TBBA) was used as a derivatization agent for the assignment of absolute configuration β-chiral primary alcohols. The structures varied from simple aliphatic alcohols to complex cyclic systems and highly substituted sugar derivatives. NMR-based method successfully implemented evaluate 17 compounds displayed ΔδPM values higher than 0.1 ppm in most cases, which makes TBBA superior MTPA MPA comparable 9-AMA.
Abstract The first nitration of codeine by using bismuth nitrate pentahydrate under mild reaction conditions is described. resulting 1‐nitrocodeine was reduced to 1‐aminocodeine, a key precursor for the synthesis azo derivative and several hydrazones. Structures both 1‐aminocodeine were unequivocally determined single‐crystal X‐ray analysis. reported preliminary synthetic study lays groundwork modified derivatives with potential biological activity.
The three-step synthesis of 4-benzyl-1H-pyrazole-3,5-diamines 2 from commercially available aldehydes 3 is given.The Knoevenagel condensation was utilized to assemble the initial carbon framework, resulting in benzylidenemalononitriles 4 which were directly transformed by reduction electron deficient C=C bond benzylmalononitriles 5. Subsequent cycloaddition hydrazine with 5 afforded desired pyrazoles 2. Due high similarity 4-arylazo-1H-pyrazole-3,5-diamines, biological activities evaluated...