A5051942157- Synthesis and biological activity
- Synthesis and Characterization of Heterocyclic Compounds
- Synthesis and Reactions of Organic Compounds
- Synthesis of heterocyclic compounds
- X-ray Diffraction in Crystallography
- Crystallization and Solubility Studies
- Synthesis and Reactivity of Sulfur-Containing Compounds
- Synthesis of Organic Compounds
- Synthesis and Biological Evaluation
- Free Radicals and Antioxidants
- Bioactive Compounds and Antitumor Agents
- Quinazolinone synthesis and applications
- Chemical synthesis and pharmacological studies
- Computational Drug Discovery Methods
- Organic Chemistry Cycloaddition Reactions
- Nanoparticle-Based Drug Delivery
- Crystallography and molecular interactions
- Eicosanoids and Hypertension Pharmacology
- Phenothiazines and Benzothiazines Synthesis and Activities
- Cancer therapeutics and mechanisms
- Cancer Mechanisms and Therapy
- Scientific Research and Studies
- Analytical Methods in Pharmaceuticals
- Structural and Chemical Analysis of Organic and Inorganic Compounds
- Sulfur-Based Synthesis Techniques
Danylo Halytsky Lviv National Medical University
2015-2024
Lviv Polytechnic National University
2014
Institute of Bioorganic Chemistry
2002
The synthesis and antitumor activity screening of novel 3-[2-(3,5-diaryl-4,5-dihydropyrazol-1-yl)-4-oxo-4,5-dihydro-1,3-thiazol-5-ylidene]-2,3-dihydro-1H-indol-2-ones 1-23 3-(3,5-diarylpyrazol-1-yl)-2,3-dihydro-1H-indol-2-ones 24-39 are performed. In vitro anticancer the synthesized compounds was tested by National Cancer Institute. Most them displayed on leukemia, melanoma, lung, colon, CNS, ovarian, renal, prostate, breast cancers cell lines. structure-activity relationship is discussed....
The potential of 4-thiazolidones (2,4-thiazolidinediones, 2-thioxo(imino)-4-thiazolidones) as drugs is under consideration by the pharmaceutical science since beginning XX century. During recent years a new phase has been seen in this field. Centerarian history synthetic research possibilities these heterocycles lead to diversity modelling biologically active compounds using 4-thiazolidone scaffolds. Modification 4- thiazolidone cycle on 2-, 3-, or 5-position successful achieve products with...
The synthesis and antitumor activity screening of novel isatin based conjugates with thiazolidine pyrazoline moieties were performed. Reaction 3,5-diaryl-4,5-dihydropyrazoles chloroacetyl chloride yielded starting 2-chloro-1-(3,5-diaryl-4,5-dihydropyrazol-1-yl)-ethanones which utilized in alkylation 5-bromoisatin. Thus, corresponding 1-[2-(3,5-diaryl-4,5-dihydropyrazol-1-yl)-2-oxoethyl]-1H-indole-2,3-diones (1a-1d) have been obtained. compounds 1a-1d used Knoevenagel condensation...
Keywords: synthesis, 4-thia(imida)zolidinones, thiopyrano[2,3-d]thiazoles, anticancer activity, (Q)SAR
2‐(4,5‐Dihydropyrazol‐1‐yl)‐thiazol‐4‐ones ( 2–5 ) have been synthesized starting from 3‐phenyl‐5‐aryl‐1‐thiocarbamoyl‐2‐pyrazolines via [2+3]‐cyclization with 2‐bromopropionic acid, maleic anhydride, N ‐arylmaleimides, and aroylacrylic acids. The in vitro anticancer activity of 2a , 3a 4a 5b 5c were tested by the National Cancer Institute. Compounds demonstrated selective inhibition leukemia cell lines growth at a single concentration (10 −5 M). screening antiviral for broad panel viruses...
A series of new 2-{4-oxo-2-[(4-oxothiazolidin-2-ylidene)-hydrazono]-thiazolidin-5-yl}-N-arylacetamides ( 4a–e ), 5-(2-oxo-2-aryl-ethyl)-2-[(4-oxothiazolidin-2-ylidene)-hydrazono]-thiazolidine-4-ones 5a–d 2-(4-oxo-2-[(2-oxothiazolidin-4-ylidene)-hydrazono]-thiazolidin-5-yl)-N-arylacetamides 7a–e and 5-(2-oxo-2-aryl-ethyl)-2-[(2-oxothiazolidin-4-ylidene)-hydrazono]-thiazolidine-4-ones 8a–d ) have been synthesized starting from 2-thioxothiazolidin-4-one 4-thioxothiazolidin-2-one through a...
GRAPHICAL ABSTRACTSynthesis, anticancer and antiviral activities of novel thiopyrano[2,3-d]thiazole-6-carbaldehydesAll authorsAndrii Lozynskyi, Sergii Golota, Borys Zimenkovsky, Dmytro Atamanyuk, Andrzej Gzella & Roman Lesykhttps://doi.org/10.1080/10426507.2016.1166108Published online:11 July 2016
AimTo evaluate the cytotoxic action of 4-thiazolidinone derivatives (ID 3288, ID 3882, and 3833) toward rat glioma C6 cells to compare effects these compounds doxorubicin on balance free radical oxidation (FRO) antioxidant activity (AOA) in serum rats.MethodsGlioma were treated with 3833, doxorubicin, their cytotoxicity was studied using MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay Trypan blue exclusion test, light fluorescent microscopy, flow cytometric study...
The series of 9,14-disubstituted 3,7-dithia-5,14-diazapentacyclo[9.5.1.02, 10.04, 8.012, 16]heptadecen-4(8)-triones-6, 13, 15 were synthesized using hetero-Diels-Alder reactions starting from 4-thioxo-2-thiazolidinones and 5-norbornene-2,3-dicarboxylic acid imido-derivatives. Screening anticancer activity in vitro yielded the most active compounds 5c, 5d, 7b micromolar concentrations at GI50 level (LogGI50 is−6.40 to−4.02 for different cell lines, LogGI50 mean graph midpoint varies from−4.67...
Abstract 5-Ethoxymethylidene-4-thioxo-2-thiazolidinone was studied as versatile core building block in the synthesis of new thiopyrano[2,3-d]thiazole derivatives relevant for medicinal chemistry purposes under hetero-Diels–Alder reaction conditions. Promising compounds (6, 10) were identified among synthesized series with high antitumor and moderate antiviral activity. [Supplementary materials are available this article. Go to publisher's online edition Synthetic Communications® following...
The synthesis and antitumor activity screening of 4-aminothiazol-2(5H)-one derivatives were performed. absence possible 4-amino-imino tautomerism thiazolidinones-2 has been confirmed based on the study molecule structures. existence alone amino-form was confirmed. An anticancer performed within Developmental Therapeutics Program (National Cancer Institute/NIH, USA). Tested compounds possess low to moderate (average values - 60 cancer cell lines assay) with significant selective action...
Abstract Novel rel -(5 R ,6 S ,7 )-2-oxo-5,7-diaryl-3,5,6,7-tetrahydro- 2H -thiopyrano[2,3- d ]thiazol-6-yl-oxo-acetic acids were synthesized in 52–70% yields via regioselective and diastereoselective hetero -Diels-Alder reaction of 5-arylidene-4-thioxo-2-thiazolidinones with a series arylidene pyruvic acids. The compounds evaluated for anticancer activity NCI60 cancer cell lines antiexudative on the carrageenan edema model rats. Biological screening data led to identification 3e as having...
AimTo compare various pro-apoptotic effects of synthetic 4-thiazolidinone derivative (Les-3288), doxorubicin (Dox) and temozolomide (TMZ) in the treatment human glioma U251 cells to improve outcomes glioblastoma avoid anticancer drug resistance.MethodsThe cytotoxic drugs used were measured by cell viability proliferation assay (MTT), Trypan blue exclusion test, Western-blot analysis apoptosis-related proteins. In addition, flow cytometry study reactive oxygen species (ROS) level was carried...
To evaluate cytotoxic action of 4-thiazolidinone derivative Les-3833 and study the mechanisms its pro-apoptotic toward human melanoma cells tumor cell lines other tissue origin.The effect or doxorubicin on viability 9 was studied using MTT assay, while WM793 line were additionally examined light fluorescent microscopies for evaluating cytomorphological changes. The Western-blot flow cytometric analyses carried out to signaling pathways cycling death.Les-3833 most efficient against cells. Its...