A5073789336- Synthesis of Organic Compounds
- Carbohydrate Chemistry and Synthesis
- Bioactive natural compounds
- Synthesis of Indole Derivatives
- Bioactive Compounds and Antitumor Agents
- Multicomponent Synthesis of Heterocycles
- Fluorine in Organic Chemistry
- Synthesis and biological activity
- Microbial Natural Products and Biosynthesis
- Natural product bioactivities and synthesis
- Biological Activity of Diterpenoids and Biflavonoids
- Chemical Synthesis and Analysis
- Glycogen Storage Diseases and Myoclonus
- Synthesis and Biological Evaluation
- Amino Acid Enzymes and Metabolism
- Synthesis and Characterization of Heterocyclic Compounds
- Chemical synthesis and alkaloids
- Oxidative Organic Chemistry Reactions
- Catalytic Alkyne Reactions
- Phenothiazines and Benzothiazines Synthesis and Activities
- Agricultural Productivity and Crop Improvement
- Click Chemistry and Applications
- Agriculture and Biological Studies
- Pharmacological Effects of Natural Compounds
- Chromatography in Natural Products
Institute of Bioorganic Chemistry and Petrochemistry V.P. Kukhar
2013-2024
National Academy of Sciences of Ukraine
2013-2023
National University of Food Technologies
2020-2021
Kyiv City Clinical Oncology Center
2015
The overaccumulation of glycogen appears as a hallmark in various storage diseases (GSDs), including Pompe, Cori, Andersen, and Lafora disease. Accumulating evidence suggests that suppression accumulation represents potential therapeutic approach for treating these GSDs. Using fluorescence polarization assay designed to screen inhibitors the key synthetic enzyme, synthase (GS), we identified substituted imidazole,...
Abstract The regioselective condensations of various 7‐hydroxyisoflavonoids with bis( N , ‐dimethylamino)methane in a Mannich reaction provided C‐8 ‐dimethylaminomethyl‐substituted isoflavonoids good yield. Similar 7‐hydroxy‐8‐methylisoflavonoids led to the C‐6‐substituted analogs. Thermal eliminations dimethylamine from these C‐6 or generated ortho ‐quinone methide intermediates within isoflavonoid frameworks for first time. Despite other potential competing outcomes, trapped dienophiles...
C-6 and C-8 Hydroxy-, acetoxy- alkoxymethyl derivatives of isoflavones were synthesized from Mannich bases show inhibition in the low micromolar range a prostate cancer PC3 cell line.
A reliable method for the synthesis of B-ring hydroxylated homoisoflavonoids and 3-hetarylmethyl chromones has been developed. The involves an initial oxa-Diels–Alder reaction ortho-quinone methides generated from aryl/hetaryl-substituted ortho-(N,N-dimethylaminomethyl)phenols with (2E)-3-(N,N-dimethylamino)-1-(2-hydroxyphenyl)prop-2-en-1-ones subsequent cascade reactions. This synthetic strategy avoids conventional multistep protocols does not require protection hydroxyl groups, thus...
The comparative analysis of the stimulating effect low molecular weight heterocyclic compounds, derivatives pyrimidine, pyrazole, isoflavones, pyridine, oxazolopyrimidine, oxazole and plant hormones auxins IAA (1H-Indol-3-ylacetic acid) NAA (1-Naphthylacetic on germination seeds growth seedlings flax (Linum usitatissimum L.) cultivars Ukrainian 3 Svitanok was conducted.The specific auxin-like chemical compounds basic processes growth: cell division, proliferation, elongation differentiation...
Chromones play an important role in the design and discovery of new pharmacologically active compounds. A large volume reports dedicated to synthesis study properties nitrogen-containing chromone derivatives show alkaloid-like The present review covers achievements field aminomethyl as one perspective scaffolds.
As part of a program focused on the development new antineoplastic agents based scaffolds found in natural products, we explored isoflavone family as potential enzyme inhibitors. We required biotin‐modified isoflavones to identify biological targets, and selected C‐2 position an attachment site for alkyl group bearing terminal carboxylic acid which could attach biotin derivative. The base‐catalyzed condensation 2,4‐dihydroxy‐substituted deoxybenzoins with cyclic anhydrides mediated by...
In this article, photoactive alkyl and aryl α-ketophosphonate derivatives were studied as inhibitors of glutathione S-transferases (GSTs). The monoesters synthesized by sodium iodide-induced dealkylation corresponding phosphonate diesters. compounds being inactive toward the enzyme without UV light activated irradiation at 365 nm which caused inhibition GSTs from equine liver human placenta with micromolar IC50 values. Hetaryl can also be potential candidates for UV-dependent targeting....
Abstract A simple and efficient method for the synthesis of 2‐(3,3,3‐trifluoroacetonyl) chromones isoflavones has been developed. This involves an initial in situ generation vinyl ethers from 2‐methyl‐ or 2‐ethylchromones/isoflavones their subsequent acylation with trifluoroacetic anhydride presence CF 3 COOK. pathway provides convenient access to novel fluorinated analogs naturally occurring chromones.
We demonstrate a protocol for the synthesis of benzopyrone-azole hybrids in reaction pyrazoles and (benz)imidazole with phenolic Mannich bases. The target compounds were studied as inhibitors α-glucosidase.
An efficient approach has been developed for the trapping in situ generated benzopyrone-based ortho-quinone methide intermediates by 3- and 5-amino pyrazoles or isoxazoles. In cases of naturally occurring phenolic Mannich bases, hybrid compounds between azole flavonoid, namely, coumarin, chromone, isoflavone, aurone were synthesized moderate to good yields. It is remarkable that depending on 5-position amino group, reaction led formation C-4 3-NH substituted derivatives, respectively. vitro...
QSAR analysis of previously synthesized and nature-inspired virtual isoflavone-cytisine hybrids against the HEp-2 laryngeal carcinoma cell lines was performed using OCHEM web platform. The validation models an external test set proved that can be used to predict activity newly designed compounds such as 8-cytisinylmethyl derivatives 5,7- 6,7-dihydroxyisoflavones. synthetic procedure for selective aminomethylation 5,7-dihydroxyisoflavones with cytisine developed. In vitro testing identified...
Mannich aminomethylation of 8-methyl-7-hydroxy-2'-fluoroisoflavones applying bis-(N,N-dimethylamino)methane afforded C-6 substituted N,N-dimethylaminomethyl derivatives. Subsequent acetylation these compounds in acetic anhydride the presence potassium acetate provided access to corresponding acetoxymethyl derivatives that were converted hydroxymethyl- and alkoxymethyl-substituted 7-hydroxyisoflavonoids. Addition 3-(N,N-dimethylamino)-5,5-dimethyl-2-cyclohexen-1-one or...