A5015194739- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Chemical Reaction Mechanisms
- Axial and Atropisomeric Chirality Synthesis
- Molecular spectroscopy and chirality
- Synthesis of Organic Compounds
- Synthetic Organic Chemistry Methods
- Carbohydrate Chemistry and Synthesis
- Sulfur-Based Synthesis Techniques
- Advanced Breast Cancer Therapies
- Organic Chemistry Cycloaddition Reactions
- Cancer-related Molecular Pathways
- Protein Degradation and Inhibitors
- Phenothiazines and Benzothiazines Synthesis and Activities
- Asymmetric Synthesis and Catalysis
Palacký University Olomouc
2021-2025
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...
A new type of axially chiral sulfonic acid was developed. The synthesis is based on cheap commercially available materials and a practical method for optical resolution via diastereomeric salt formation, which can provide both enantiomers. Eleven benzoimidazolylnaphthalenesulfonic acids were prepared four them isolated as pure stable atropisomers. Moreover, several these transformed into triflyl imides to further expand the range dissociation constants.
Cycle-regulating and transcriptional cyclin-dependent kinases (CDKs) are attractive targets in cancer drug development. Several CDK inhibitors have already been obtained or close to regulatory approval for clinical applications.Phenylazopyrazole CAN508 has described as the first selective CDK9 inhibitor with an IC50 of 350 nM. Since azo-moiety is not a suitable functionality drugs due pharmacological reasons, preparation carbo-analogues similar biological activities desirable. The present...
Abstract The novel synthesis of unsymmetrical 1,1’‐bibenzimidazoles is described. key N−N bond was introduced on 1H ‐benzimidazole or ‐benzimidazole‐2‐sulfonic acid by N‐amination with hydroxylamine‐ O ‐sulfonic (HASA). precursors, 1‐[(2‐nitrophenyl)amino]‐ ‐benzimidazoles, were prepared nucleophilic aromatic substitution 1‐fluoro‐2‐nitrobenzene ‐benzimidazole‐1‐amines. demonstrated 11 1,1’‐bibenzimidazoles, which in the final step one‐pot reduction/cyclization DMF DMA acetals under mild...