A5091741382- Histone Deacetylase Inhibitors Research
- Protein Degradation and Inhibitors
- Various Chemistry Research Topics
- Signaling Pathways in Disease
- Peptidase Inhibition and Analysis
- Genomics, phytochemicals, and oxidative stress
- Free Radicals and Antioxidants
- Molecular spectroscopy and chirality
- Phytochemical compounds biological activities
- Plant chemical constituents analysis
- Innovative Teaching Methods
- Analytical Chemistry and Chromatography
- Chemical Reaction Mechanisms
- Cancer Mechanisms and Therapy
- Phytochemistry and Biological Activities
Heinrich Heine University Düsseldorf
2016-2021
Inhibition of more than one cancer-related pathway by multi-target agents is an emerging approach in modern anticancer drug discovery. Here, based on the well-established synergy between histone deacetylase inhibitors (HDACi) and alkylating agents, we present discovery a series HDACi using pharmacophore-linking strategy. For parallel synthesis target compounds, developed efficient solid-phase-supported protocol hydroxamic acids immobilized resins (HAIRs) as stable versatile building blocks...
High grade serous ovarian cancer (HGSOC) is the most common and aggressive subtype with worst clinical outcome due to intrinsic or acquired drug resistance. Standard treatment involves platinum compounds. Cancer development chemoresistance often associated an increase in histone deacetylase (HDAC) activity. The purpose of this study was examine potential HDAC inhibitors (HDACi) potency HGSOC. Four HGSOC cell lines different cisplatin sensitivity were treated combinations entinostat (class I...
Nuclear magnetic resonance (NMR) spectroscopy is a widely used analytical technique for molecular structure determination, and highly valued in the fields of chemistry, biochemistry, medicinal chemistry. The importance NMR methods European (PhEur) United States Pharmacopeia (USP) steadily growing. However, undergraduates often have problems becoming familiar with handling complex data. We developed simple experiment which undergraduates, who are learning 1H first time, investigate natural...
Marketed pain relief drugs with one to three biologically active components, as well mixtures of these ingredients, were qualitatively and quantitatively analyzed in an undergraduate student lab using a compact, low-field 1H NMR spectrometer. The students successfully more than 50 self-made sample two or components the marketed tablet formulations containing acetylsalicylic acid/l-ascorbic acid, acid/paracetamol (acetaminophen)/caffeine. NMR-based quantification is attractive application...
Ovarian cancer is the fifth leading cause of deaths. Chemoresistance, particularly against platinum compounds, contributes to a poor prognosis. Histone deacetylase inhibitors (HDACi) and heat shock protein 90 (HSP90i) are known modulate pathways involved in chemoresistance. This study investigated effects HDACi (panobinostat, LMK235) HSP90i (luminespib, HSP990) on potency cisplatin ovarian cell lines (A2780, CaOV3, OVCAR3 cisplatin-resistant sub-clones). Preincubation with increased...
For an interdisciplinary approach on different topics of medicinal and analytical chemistry, we applied a known experimental pKa value determination method the field bench top nuclear magnetic resonance (NMR) spectrometry some biologically active pyridine-based drugs, i.e., pyridoxine hydrochloride, isoniazid, nicotine amide. The chemical shifts aromatic ring protons in 1H NMR spectrum change depending protonation status. data were analyzed dependence by pH (pD) environments then values...
The dichloromethane extract from leaves of Melicope barbigera (Rutaceae), endemic to the Hawaiian island Kaua’i, yielded four new and three previously known acetophenones 2H-chromenes, all found for first time in M. barbigera. structures compounds obtained after purification by chromatographic methods were unambiguously elucidated spectroscopic analyses including 1D/2D NMR spectroscopy HRESIMS. absolute configuration was determined modified Mosher’s method. Compounds 2, 4 mixture 6 7...
Abstract Multi‐Target‐Wirkstoffe stellen in der modernen Tumortherapie einen vielversprechenden Ansatz dar. Basierend auf dem bekannten Synergismus zwischen Histon‐Deacetylase‐Inhibitoren (HDACi) und alkylierenden Zytostatika präsentieren wir dieser Arbeit die Entwicklung von HDACi, welche aus einer Pharmakophor‐Verknüpfungsstrategie hervorgegangen sind. Für Synthese haben ein Protokoll entwickelt, bei Hydroxamsäuren an Festphasenharze immobilisiert als vielseitig anwendbare Bausteine für...