A5088690369- Phenothiazines and Benzothiazines Synthesis and Activities
- Synthesis and biological activity
- Inflammatory mediators and NSAID effects
- Analytical Chemistry and Chromatography
- Terahertz technology and applications
- Lipid Membrane Structure and Behavior
- Synthesis and Biological Evaluation
- Crystallization and Solubility Studies
- Quinazolinone synthesis and applications
- thermodynamics and calorimetric analyses
- Computational Drug Discovery Methods
- Synthesis and Reactivity of Heterocycles
- X-ray Diffraction in Crystallography
- Chemical synthesis and pharmacological studies
- Cancer, Stress, Anesthesia, and Immune Response
- Structural and Chemical Analysis of Organic and Inorganic Compounds
- Heat shock proteins research
- Chemical Reaction Mechanisms
- Veterinary medicine and infectious diseases
- Chemokine receptors and signaling
- Cancer therapeutics and mechanisms
- Allergic Rhinitis and Sensitization
- NF-κB Signaling Pathways
- Tryptophan and brain disorders
- Advanced Chemical Sensor Technologies
Wroclaw Medical University
2015-2024
National Institute of Standards and Technology
2023
Université de Lorraine
2023
Medical University of Silesia
2020
Heat shock proteins HSPA1/Hsp70α and HSP90AA1/Hsp90α are crucial for cancer growth but their expression pattern in colorectal polyps or whether they can be modulated by oxicams is unknown. We quantified (RTqPCR) HSPA1 HSP90AA1 50 polyp-normal pairs relation to polyp malignancy potential examined the effect of piroxicam, meloxicam five novel analogues on (mRNA/protein) adenocarcinoma lines. were upregulated 3- 2.9-fold. Expression ratios higher with dysplasia grade dominant villous pattern,...
The aim of this study was to obtain new, safe, and effective compounds with anticancer activity since cancer is still the leading cause mortality worldwide. rational design new based on introduction differentially substituted phenylpiperazines into 1,2-benzothiazine scaffold as a reference for structures recent topoisomerase II (Topo II) inhibitors such dexrazoxane XK-469. newly designed group derivatives synthesized tested healthy (MCF10A) (MCF7) cell lines, alone in combination doxorubicin...
L-arginine/nitric oxide pathway metabolites are altered in colorectal cancer (CRC). We evaluated underlying changes enzymes 55 paired tumor/tumor-adjacent samples and 20 normal mucosa using quantitative-PCR assessed the impact of classic novel oxicam analogues on enzyme expression intracellular metabolite concentration (LC-MS/MS) Caco-2, HCT116, HT-29 cells. Compared to mucosa, ARG1, PRMT1, PRMT5 were overexpressed both tumor tumor-adjacent tissue DDAH2 solely tissue. Tumor-adjacent had...
Oxicams (e.g. piroxicam, meloxicam) are widely used nonsteroidal anti-inflammatory drugs (NSAIDs). A large body of evidence from epidemiological and preclinical studies has shown that NSAIDs have a chemopreventive effect on different types cancer, especially in colorectal cancer. Moreover, mounting clinical suggests persistent inflammation functions as driving force the journey to What is more, induces reactive oxygen nitrogen species, which cause damage important cellular components (e.g.,...
Incidence of cancer is still increasing. Chemotherapy often unsuccessful; moreover, anticancer drugs cause serious side-effects. It necessary to develop effective agents for combination therapies that would increase antitumor effects treatment and reduce its side-effects.Anticancer activity oxicam derivatives (PR17 PR18) alone in with simvastatin on doxorubicin-resistant colon cells was studied. Apoptosis investigated via caspase-3 activation assay as well western blot analysis expression...
A series of potential biologically active 2-[3-(4-phenyl-1-piperazinyl)propyl]-3-(4-substituted-benzoyl)-4-hydroxy-2H-1,2-benzothiazine 1,1-dioxides was synthesized in a straightforward manner by condensation respective 3-substituted-4-hydroxy-1,2-benzothiazine with 1-(1-chloropropyl)-4-phenylpiperazine. The structures all the newly formed compounds were identified elemental analysis, FTIR and 1H NMR. subjected to preliminary evaluation using differential scanning calorimetry (DSC) determine...
The global concern related with growing number of bacterial pathogens, resistant to numerous antibiotics, prone scientific environment search for new antimicrobials. Antiseptics appear be suitable candidates as adjunctive agents antibiotics or alternative local treatment option aiming prevent and treat infections. 1,2-benzothiazines are considered one the most promising them. In this research twenty 1,2-benzothiazine 1,1-dioxide derivatives were scrutinized regard their biological activity....
Abstract In this paper we discuss the link between domain of physical parameters – molecular descriptors a drug, and terahertz (THz) spectra. We measured derivatives well-known anti-inflammatory drug Piroxicam using THz spectroscopy employed Principal Component Analysis to build similarity maps in descriptor spectral domains. observed, that spatial neighborhood on map is highly correlated with neighbourhood within group structurally-similar molecules. built Partial Least Squares (PLS)...
The purpose of the present paper was to assess ability five newly designed and synthesized meloxicam analogues interact with phospholipid bilayers. Calorimetric fluorescence spectroscopic measurements revealed that, depending on details chemical structure, studied compounds penetrated bilayers affected mainly their polar/apolar regions, closer surface model membrane. influence thermotropic properties DPPC clearly visible because these reduced temperature cooperativity main phase transition....
The purpose of the present work was to assess ability five new oxicam analogues interact with lipid bilayers. To characterize interaction newly synthesized NSAIDs (non-steroidal anti-inflammatory drugs) DPPC bilayers two following techniques were applied - differential scanning calorimetry (DSC) and fluorescence spectroscopy. results obtained by these experimental approaches show that oxicams model membranes under consideration. As demonstrated both in calorimetric spectroscopic studies,...
The series of three 4-alkoxy-2-[2-hydroxy-3-(4-aryl-1-piperazinyl)propyl]-6-methyl-1H-pyrrolo[3,4-c]pyridine-1,3(2H)-diones were synthesized. structures all formed compounds identified by elemental analysis, FTIR, and 1H NMR. synthesized studied using differential scanning calorimetry thermogravimetric analysis in order to determine the existence multiple solid-state forms. Our measurements showed that solvent, mechanical treatment, quenching are important factors. Two stable one metastable...
Alzheimer's disease (AD) is considered the most common cause of dementia among elderly. One modifiable causes AD neuroinflammation. The current study aimed to investigate influence new tricyclic 1,2-thiazine derivatives on in vitro model neuroinflammation and their ability cross blood-brain barrier (BBB). potential anti-inflammatory effect (TP1, TP4, TP5, TP6, TP7, TP8, TP9, TP10) was assessed SH-SY5Y cells differentiated neuron-like phenotype incubated with bacterial lipopolysaccharide (5...
New, tricyclic compounds containing a sulfonyl moiety in their structure, as potential safer COX inhibitors, were designed and synthesized. New derivatives have three conjugated rings group. A third ring, i.e., an oxazine, oxazepine or oxazocin, has been added to the 1,2-benzothiazine skeleton. Their anti-COX-1/COX-2 cytotoxic effects vitro on NHDF cells, together with ability interact model membranes influence reactive oxygen species nitric oxide, studied. Additionally, molecular docking...
The new derivatives of 3,4-pyridinedicarboximide were synthesised. Experimental measurements carried out using 1H NMR spectra, IR elemental analyses and differential scanning calorimetry. purpose this study was to the thermal stability these four compounds establish a solid-state polymorphism. Measurements for samples obtained from ethanol n-hexane after long-time storage.
In this paper we report a new approach to linking the terahertz spectral shapes of drug candidates having similar molecular structure their chemical and physical parameters. We examined 27 newly-synthesized derivatives well-known nonsteroidal anti-inflammatory Piroxicam used for treatment inflammatory arthritis chemoprevention colon cancer. The testing was carried out by means pulsed spectroscopy (TPS). Using chemometric techniques evaluated similarity in range attempted link position on...
The mechanisms underlying the antineoplastic effects of oxicams have not been fully elucidated. We aimed to assess effect classic and novel on expression/secretion macrophage-associated chemokines (RTqPCR/Luminex xMAP) in colorectal adenocarcinoma cells, expression upstream non-steroidal anti-inflammatory drug (NSAID)-activated genes NAG1, NFKBIA, MYD88, RELA, as well at chemokine profiling tumors. Meloxicam downregulated CCL4 9.9-fold, but otherwise had a negligible/non-significant effect....
The drug interactions with the lipid membranes are crucial in many biochemical processes. Phospholipid model often used to assess such interactions. Our team has been researching new compounds anti-inflammatory and analgesic effects for years. Such derivatives of well-known non-steroidal (NSAID) - meloxicam (MLX). Their biological target is cyclooxygenase (COX) a membrane protein. NSAIDs mainly taken orally; therefore, drug-membrane interaction preliminary stage body.
The design of novel anti-inflammatory drugs remains a critical area research in the development effective treatments for inflammatory diseases. In this study, series 1,2-benzothiazine was evaluated through multifaceted approach. particular, we investigated potential interactions with lipid bilayers, an important consideration membrane permeability and overall pharmacokinetics. addition, their ability to inhibit cyclooxygenase 1 2 activity selectivity using both inhibition assay molecular...
Polymorphic conversion is a major concern of the pharmaceutical industry. Therefore, it essential to characterize and quantify polymorphic forms drugs. Vibrational spectroscopic techniques such as infrared, near-infrared, Raman and, most recently, terahertz pulsed spectroscopy have become popular for solid state analysis since they are fast non-destructive allow solid-state changes be probed at molecular level. We synthesized investigated new derivatives known anti-inflammatory drug...
The modified 1,2-benzothiazine analogues designed as new drug candidates and discussed in this paper are oxicam derivatives. Oxicams a class of non-steroidal anti-inflammatory drugs (NSAIDs). Their biological target is cyclooxygenase (COX), membrane protein associated with the phospholipid bilayer. In recent decades, it has been proven that effect NSAIDs may be closely related to their interaction at level membrane. These processes often complicated membranes themselves very complex....