A5039492413- Synthesis and biological activity
- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Synthesis and Characterization of Heterocyclic Compounds
- Click Chemistry and Applications
- Metal complexes synthesis and properties
- Synthesis of heterocyclic compounds
- Synthesis and Biological Evaluation
- Photodynamic Therapy Research Studies
- Nanoplatforms for cancer theranostics
- Crystallography and molecular interactions
- Synthesis and Reactivity of Sulfur-Containing Compounds
- Ferrocene Chemistry and Applications
- Multicomponent Synthesis of Heterocycles
- Computational Drug Discovery Methods
- Histone Deacetylase Inhibitors Research
- Photochromic and Fluorescence Chemistry
- Pharmacogenetics and Drug Metabolism
- Synthesis and Reactions of Organic Compounds
- Cancer, Hypoxia, and Metabolism
- Drug Transport and Resistance Mechanisms
- Inflammatory mediators and NSAID effects
- Organometallic Complex Synthesis and Catalysis
- Fluorine in Organic Chemistry
- Research on Leishmaniasis Studies
North Carolina State University
2024-2025
University of Kentucky
2016-2023
Dragomanov Ukrainian State University
2020
Danylo Halytsky Lviv National Medical University
2008-2017
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....
Ru(II) complex photocages are used in a variety of biological applications, but the thermal stability, photosubstitution quantum yield, and compatibility most commonly systems remain unoptimized. Here, multiple compounds photocaging applications were analyzed found to have several unsatisfactory characteristics. To address these deficiencies, three new scaffolds designed improve key properties through modulation combination electronic, steric, physiochemical features. One systems, containing...
Abstract The cytochrome P450 family of enzymes (CYPs) are important targets for medicinal chemistry. Recently, CYP1B1 has emerged as a key player in chemotherapy resistance the treatment cancer. This enzyme is overexpressed variety tumors, and correlated with poor outcomes; thus, it desirable to develop inhibitors restore efficacy. However, possible off-target effects, such inhibition liver CYPs responsible first pass metabolism, make selective high priority avoid drug-drug interactions...
Hyperpolarization derived from signal amplification by reversible exchange (SABRE) is valued for its relative simplicity among hyperpolarization approaches. Here, we demonstrate that photoejection of the ligands pyridazine and pyrazine prodrug Ru(II) polypyridyl complexes offers a new modality activating SABRE hyperpolarization, achieving enhancements over 3200-fold.
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...
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...
Ruthenium complexes capable of light‐triggered cytotoxicity are appealing potential prodrugs for photodynamic therapy (PDT) and photoactivated chemotherapy (PACT). Two groups (polypyridyl)Ru II with 2‐(2‐pyridyl)benzazole ligands were synthesized investigated their photochemical properties anticancer activity to compare strained unstrained systems that likely have different biological mechanisms action. The structure–activity relationship was focused on the benzazole‐core bioisosterism...
A series of strained Ru(II) complexes were studied for potential anticancer activity in hypoxic tissues. The constructed with methylated ligands that photolabile and an imidizo[4,5-f][1,10]phenanthroline ligand contained appended aromatic group to potentially allow contributions ligand-centered excited states. systematic variation the size energy was performed using systems containing 1-4 fused rings, photochemical photobiological behaviors all assessed. structure nature had a subtle impact...
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...
Coordination complexes can be used to photocage biologically active ligands, providing control over the location, time, and dose of a delivered drug.
Abstract In an earlier study of π‐expansive ruthenium complexes for photodynamic and photochemo‐therapies, it was shown that a pair structural isomers differing only in the connection point naphthalene residue exhibited vastly different biological activity. These are further explored this paper through activity their functionalized derivatives. normoxia, inactive 2‐NIP isomer ( 5 ) can be made as photocytotoxic active 1‐NIP 1 by functionalizing with methyl or methoxy groups, while variants...
While cytochrome P450 (CYP; P450) enzymes are commonly associated with the metabolism of organic xenobiotics and drugs or biosynthesis signaling molecules, they also impacted by a variety inorganic species. Metallic nanoparticles, clusters, ions, complexes can alter CYP expression, modify enzyme interactions reductase partners, serve as direct inhibitors. This overlooked topic is reviewed here, an emphasis on understanding structural physiochemical basis for these interactions. Intriguingly,...
The discovery of new light-triggered prodrugs based on ruthenium (II) complexes is a promising approach for photoactivated chemotherapy (PACT). light-mediated activation "strained" Ru(II) polypyridyl resulted in ligand release and produced ligand-deficient metal center capable forming covalent adducts with biomolecules such as DNA. Based the strategy exploiting structural distortion to activate photochemistry, biologically active small molecules were coordinated scaffold create dual-action...
Ruthenium complexes are often investigated as potential replacements for platinum-based chemotherapeutics in hopes of identifying systems with improved tolerability vivo and reduced susceptibility to cellular resistance mechanisms. Inspired by phenanthriplatin, a non-traditional platinum agent that contains only one labile ligand, monofunctional ruthenium polypyridyl agents have been developed, but until now, few demonstrated promising anticancer activity. Here we introduce potent new...
The features of the chemistry 4-thiazolidinone and isatin as privileged scaffolds were described in a number reviews which main approaches to synthesis mentioned heterocycles their pharmacological action analyzed. However, 4-thiazolidinone-indoline conjugates well based heterocyclic hybrids biologically active compounds is poorly discussed context pharmacophore hybrid approach. Therefore, purpose this review summarize data about biological activity systems with thiazolidinone 2-oxoindoline...