A5021941013- Catalytic C–H Functionalization Methods
- Asymmetric Hydrogenation and Catalysis
- Synthesis and Catalytic Reactions
- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Catalytic Cross-Coupling Reactions
- Chemical Synthesis and Analysis
- Protein Degradation and Inhibitors
- Radical Photochemical Reactions
- Sulfur-Based Synthesis Techniques
- Synthetic Organic Chemistry Methods
- Asymmetric Synthesis and Catalysis
- Fluorine in Organic Chemistry
- Advanced Synthetic Organic Chemistry
- Catalytic Alkyne Reactions
- Peptidase Inhibition and Analysis
- Cyclopropane Reaction Mechanisms
- Chemical Synthesis and Reactions
- Chromatin Remodeling and Cancer
- Axial and Atropisomeric Chirality Synthesis
- Ubiquitin and proteasome pathways
- Innovative Microfluidic and Catalytic Techniques Innovation
- Crystallography and molecular interactions
- Synthesis and biological activity
- Synthesis of Indole Derivatives
University of Vienna
2015-2025
Boehringer Ingelheim (Austria)
2017-2024
University of Toronto
2019-2023
Université de Montréal
2019
Kansas State University
2019
Université d'Orléans
2019
University of Hassan II Casablanca
2019
Medical University of Vienna
2015
This comprehensive review, covering 2021-2023, explores the multifaceted chemical and pharmacological potential of coumarins, emphasizing their significance as versatile natural derivatives in medicinal chemistry. The synthesis functionalization coumarins have advanced with innovative strategies. enabled incorporation diverse functional fragments or construction supplementary cyclic architectures, thereby biological physico-chemical properties compounds obtained were enhanced. unique...
Focal adhesion tyrosine kinase (PTK2) is often overexpressed in human hepatocellular carcinoma (HCC), and several reports have linked PTK2 depletion and/or pharmacological inhibition to reduced tumorigenicity. However, the clinical relevance of targeting still remains be proven. Here, we present two highly selective functional proteolysis-targeting chimeras utilizing von Hippel-Lindau cereblon ligands hijack E3 ligases for degradation. BI-3663 (cereblon-based) degrades with a median DC50 30...
Abstract Cytochrome P450 (CYP) 3A4 plays a major role in drug metabolism. Its activity could be determined by non-invasive and cost-effective assays, such as breath analysis, for the personalised monitoring of response. For first time, we identify an isotopically unlabelled CYP3A4 substrate, tolterodine that leads to formation non-toxic volatile metabolite, acetone, which potentially applied monitor humans. In vitro biotransformation HepG2 cells overexpressing CYP3A4, CYP2D6 or CYP2C9 was...
Abstract Vacuoles are essential for cellular metabolism and growth the maintenance of internal turgor pressure. They sequester lytic enzymes, ions secondary metabolites that, if leaked into cytosol, could lead to cell death. Despite their pivotal roles, quality control pathways that safeguard vacuolar integrity have remained elusive in plants. Here we describe a conserved pathway is activated upon wall damage turgor-pressure-dependent manner. Cell perturbations induce distinct...
The diterpenoid alkaloids serve as a rich source of synthetic targets for organic chemists, due to the intriguing structure overlapping ring systems, along with biological activities commonly associated compounds this group. Fifteen total syntheses and numerous studies towards construction fragments have been reported since 2010. This review article gives brief overview summarizes recent efforts. 1 Introduction 1.1 Structural Classification Biosynthetic Origin 1.2 Structure Elucidation...
Herein we report a method for the synthesis of indazoles from readily available 2-aminomethyl-phenylamines via N–N bond-forming oxidative cyclization. Inspired by indazole formation initially observed as side product N. Coskun et al. developed robust protocol to access in all three tautomeric forms. The selectively gives various 2-substituted 2H-indazoles which are frequently used drug design, and also demonstrated its applicability less studied 3H-indazoles.
A dearomative electrophilic fluorination of 2-methylindoles is reported, delivering 3,3-difluoroindolines bearing an exomethylidene. The model substrate was synthesized on up to a 20 mmol scale and purified by practical recrystallization as crystalline bench-stable, yet reactive solid. olefin amphoteric can react both nucleophile electrophile. wide range metal-free, palladium, rhodium, copper reactions explored, forming new C–H, C–B, C–C (alkyl aryl), C–N, C–O, C–P, C–S bonds.
Abstract Colloidal drug aggregates enable the design of drug‐rich nanoparticles; however, efficacy stabilized colloidal is limited by entrapment in endo‐lysosomal pathway. Although ionizable drugs are used to elicit lysosomal escape, this approach hindered toxicity associated with phospholipidosis. It hypothesized that tuning p K a would endosomal disruption while avoiding phospholipidosis and minimizing toxicity. To test idea, 12 analogs nonionizable fulvestrant synthesized groups...
Histone deacetylase 6 (HDAC6) inhibition is an attractive strategy for treating numerous cancers, and HDAC6 catalytic inhibitors are currently in clinical trials. The zinc-finger ubiquitin-binding domain (UBD) binds free C-terminal diglycine motifs of unanchored ubiquitin polymer chains protein aggregates, playing important role autophagy aggresome assembly. However, targeting this with small molecule antagonists remains underdeveloped avenue HDAC6-focused drug discovery. We report...
3-Aminomethylation of salicylalkylamides afforded hybrids with a Mannich base. In addition, it triggered the rotation amide bond. The observed conformational switch is driven by strong intramolecular hydrogen bonding between base and phenolic group. Crystal structure analysis reveals stabilization hybrid molecules double OH, which acts as an acceptor donor simultaneously. contain site in orthogonal spatial arrangement. bonds are persistent nonpolar solvent (e.g., chloroform). change can be...
Vacuoles are essential for cellular metabolism, growth, and the maintenance of internal turgor pressure. They sequester lytic enzymes, ions, secondary metabolites that, if leaked into cytosol, could lead to cell death. Despite their pivotal roles, quality control pathways that safeguard vacuolar integrity remained elusive in plants. Here, we discovered a conserved (VQC) pathway is activated upon wall damage pressure dependent manner. Cell perturbations induce distinct modification -...
ABSTRACT Histone deacetylase 6 (HDAC6) inhibition is an attractive strategy for treating numerous cancers, and HDAC6 catalytic inhibitors are currently in clinical trials. The zinc-finger ubiquitin-binding domain (UBD) binds free C-terminal diglycine motifs of unanchored ubiquitin polymer chains protein aggregates, playing important role autophagy aggresome assembly. However, targeting this with small molecule antagonists remains underdeveloped avenue HDAC6-focused drug discovery. We report...
Correction to: Recent Advances Towards Syntheses of Diterpenoid AlkaloidsSynthesis eFirstDOI: 10.1055/s-0037-1611897
Key words asymmetric synthesis - axial chirality indoles cross-coupling