A5024040986- Fungal Biology and Applications
- Alkaloids: synthesis and pharmacology
- Microbial Natural Products and Biosynthesis
- Cancer Treatment and Pharmacology
- Chemical synthesis and alkaloids
- Bioactive Compounds and Antitumor Agents
- Synthesis and biological activity
- Natural product bioactivities and synthesis
- Asymmetric Synthesis and Catalysis
- Phytochemical compounds biological activities
- Phytochemistry and Bioactivity Studies
- Berberine and alkaloids research
- Plant biochemistry and biosynthesis
- Synthesis and bioactivity of alkaloids
- Insect and Pesticide Research
- Metabolomics and Mass Spectrometry Studies
- Plant-based Medicinal Research
- Cancer therapeutics and mechanisms
- Oxidative Organic Chemistry Reactions
- Chromatography in Natural Products
- Carbohydrate Chemistry and Synthesis
- Organophosphorus compounds synthesis
- Innovative Microfluidic and Catalytic Techniques Innovation
- Synthesis and Biological Evaluation
- Quinazolinone synthesis and applications
Gedeon Richter (Hungary)
2016-2025
Szent János Kórház
2024
Budapest University of Technology and Economics
1989-2020
Jasco (United Kingdom)
2020
University of Milan
2020
Enamine (Ukraine)
2020
Institute of Bioorganic Chemistry and Petrochemistry V.P. Kukhar
2020
Johannes Gutenberg University Mainz
2020
Tohoku University
2020
Semmelweis University
2000
Cancer cells generally possess higher levels of reactive oxygen species than normal cells, and this can serve as a possible therapeutic target. In proof-of-concept study, an antioxidant-inspired drug discovery strategy was evaluated using hydroxycinnamic acid derivative. The processing oxidized mixtures p-coumaric methyl ester (pcm) revealed new antitumor lead, graviquinone. Graviquinone bypassed ABCB1-mediated resistance, induced DNA damage in lung carcinoma but exerted protective activity...
Mycochemical study of the mushroom Gymnopus fusipes led to discovery two new cyclopeptides. The compounds, named as gymnopeptides A and B, are unprecedented highly N-methylated cyclic octadecapeptides. Detailed spectroscopic studies, Marfey's analysis, a preliminary molecular modeling suggested that both natural β hairpins. isolated compounds exhibited striking antiproliferative activity on several human cancer cell lines, with nanomolar IC50 values.
Bioassay-guided fractionation of the chloroform extract Tapinella atrotomentosa led to isolation four secondary metabolites 1⁻4. Two compounds are lactones—osmundalactone (1) and 5-hydroxy-hex-2-en-4-olide (2)—while 3 4 were identified as terphenyl quinones, spiromentins C B, respectively. The structures established on basis NMR MS spectroscopic analysis. isolated fungal evaluated for their antibacterial activities against several Gram-positive negative bacteria. In addition, synergistic...
A series of novel vindoline-piperazine conjugates were synthesized by coupling 6 N-substituted piperazine pharmacophores at positions 10 and 17 Vinca alkaloid monomer vindoline through different types linkers. The in vitro antiproliferative activity the new was investigated on 60 human tumor cell lines (NCI60). Nine compounds presented significant effects. most potent derivatives showed low micromolar growth inhibition (GI50) values against lines. Among them, containing...
An in-depth chemical study of the fungus Gymnopus fusipes led to discovery two new cyclooctadecapeptides, gymnopeptides C and D, besides known A B. Spectroscopic studies, as well Marfey's analysis, molecular modeling studies revealed characteristic structural features these cyclopeptides. Gymnopeptides A–D demonstrated antiproliferative activity on A375 human cancer cell line, induced apoptosis by upregulation caspase-3 activity, acted a suppressor migration.
The Vinca alkaloid vindoline was coupled at position 17 with several trisubstituted phosphine derivatives and their in vitro anticancer activities on 60 human tumor cell lines (NCI60) were investigated. This phosphonium-type ionic side chain is beneficial because it allows therapeutic molecules to pass through the membrane. Thus, candidates can exert mitochondria. coupling of phosphines achieved flexible or rigid linkers. Instead phosphonium structural part, a neutral moiety, namely...
Chrysin is a naturally occurring flavonoid with mild anticancer activity. In this paper we report the synthesis of new chrysin derivatives alkylated N-phenylchloroacetamides in position 7. A novel method was developed for preparation 7-aminochrysin via Smiles rearrangement, resulting diphenylamine-type compounds. silico studies rearrangement were performed. We also present vitro antiproliferative activity synthesized compounds against 60 human tumor cell lines (NCI60). The most potent...
Numerous honeybee products are used in medicine, but the literature furnishes no information concerning effects of drone milk (DM), although brood, which is similar to DM, was reported elicit a hormone-like strengthening effect. In certain countries, DM traditionally treat infertility and promote vitality both men women. The aim this study determine putative estrogen effect raw rats identify effective compounds. Uterotrophic assays revealed that increased relative weight immature rat uterus....
New Vinca alkaloid derivatives were synthesized to improve the biological activity of natural vindoline. To this end, experiments performed link vindoline with various structural units, such as amino acids, a 1,2,3-triazole derivative, morpholine, piperazine and N-methylpiperazine. The structure new compounds was characterized by NMR spectroscopy mass spectrometry (MS). Several exhibited in vitro antiproliferative against human gynecological cancer cell lines IC50 values low micromolar...
In this paper, we present an additional, new cage-GABA compound, called 4-amino-1-(4′-dimethylaminoisopropoxy-5′,7′-dinitro-2′,3′-dihydro-indol-1-yl)-1-oxobutane-γ-aminobutyric acid (iDMPO-DNI-GABA), and currently, compound is the only photoreagent, which can be applied for GABA uncaging without experimental compromises. By a systematic theoretical design successful synthesis of several compounds, best reagent exhibits high two-photon efficiency within 700–760 nm range with excellent...
Abstract Cariprazine—the only single antipsychotic drug in the market which can handle all symptoms of bipolar I disorder—involves trans- 4-substituted cyclohexane-1-amine as a key structural element. In this work, production trans -4-substituted cyclohexane-1-amines was investigated applying transaminases either diastereotope selective amination starting from corresponding ketone or diastereomer deamination their diasteromeric mixtures. Transaminases were identified enabling conversion cis...
Twelve compounds (1⁻12) were isolated from the methanol extract of brick cap mushroom (Hypholoma lateritium (Schaeff.) P. Kumm.). The structures elucidated using extensive spectroscopic analyses, including NMR and MS measurements. Lanosta-7,9(11)-diene-12β,21α-epoxy-2α,3β,24β,25-tetraol (1) 8-hydroxy-13-oxo-9E,11E-octa-decadienoic acid (2) identified as new natural products, together with ten known compounds, which 3β-hydroxyergosta-7,22-diene (4), demethylincisterol A2 (5), cerevisterol...
10-Bromovindoline and its 14,15-dihydro-and 14,15-cyclopropano derivatives were coupled in the position 16 with (L)-and (D)-tryptophan methyl esters.The tryptophan of vindoline synthesized starting from 16-carboxylic acid hydrazides via corresponding azides which allowed to react amino new compounds showed antitumor activity against human leukemia (HL-60) cells vitro.
The freshwater cyanobacterium Cylindrospermopsis raciborskii was investigated for carotenoid composition. Besides β-carotene, echinenone and (9/9′Z)-echinenone a glycoside found to be the main component. This compound isolated subsequently acetylated structural elucidation. acetyl derivative fully characterized by UV–vis, ECD, NMR HRMS techniques. detailed 1H 13C chemical shift assignment of major supported unequivocal identification (2′S)-2-hydroxymyxol 2′-α-l-fucoside.
The detailed chemical analysis of the methanol extract Meripilus giganteus (Pers.) P. Karst. led to isolation two new cerebrosides, mericeramides A (1) and B (2) together with cerebroside (3), ergosterol (4), 3β-hydroxyergosta-7,22-diene (5), cerevisterol (6), 3β-hydroxyergosta-6,8(14),22-triene (7), 3β-O-glucopyranosyl-5,8-epidioxyergosta-6,22-diene (8) (11E,13E)-9,10-dihydroxy-11,13-octadecadienoic acid (9). structures compounds were determined on basis NMR MS spectroscopic analysis....
Hydroxycinnamic acids represent a versatile group of dietary plant antioxidants. Oxidation methyl-p-coumarate (pcm) and methyl caffeate (cm) was previously found to yield potent antitumor metabolites. Here, we report the formation potentially bioactive products pcm cm oxidized with peroxynitrite (ONOO¯), biologically relevant reactive nitrogen species (RNS), or α,α'-azodiisobutyramidine dihydrochloride (AAPH) as chemical model for oxygen (ROS). A continuous flow system developed achieve...
Investigation of the methanol extract poroid fungus Fuscoporia torulosa resulted in isolation a novel triterpene, fuscoporic acid (1), together with inoscavin A and its previously undescribed Z isomer (2 3), 3,4-dihydroxy-benzaldehide (4), osmundacetone (5), senexdiolic (6), natalic (7), ergosta-7,22-diene-3-one (8). The structures fungal compounds were determined on basis NMR MS spectroscopic analyses, as well molecular modeling studies. Compounds 1, 6–8 examined for their antibacterial...
Metabotropic glutamate receptor 2 (mGluR2) positive allosteric modulators (PAMs) have been implicated as potential pharmacotherapy for psychiatric conditions. Screening our corporate compound deck, we identified a benzotriazole fragment (4) that was rapidly optimized to potent and metabolically stable early lead (16). The highly lipophilic character of 16, together with its limited solubility, permeability, high protein binding, however, did not allow reaching the proof concept in vivo....
Starting from racemic naringenin ((±)- 1 ), a mixture of dracocephin A stereoisomers 6-(2”-pyrrolidinone-5”-yl)naringenin (±)- 2a–d and its regioisomer, B 8-(2”-pyrrolidinone-5”-yl)naringenin 3a–d originally isolated Dracocephalum rupestre , have been synthesized in one-pot reaction. The separation was achieved by preparative HPLC. four each natural product were separated analytical chiral HPLC their absolute configuration studied the combination HPLC–ECD measurements TDDFT–ECD calculations....
Inonotus nidus-pici is a sterile conk which produces macrofungus, neglected Central-Eastern European relative of the prized obliquus, also known as chaga. Investigation methanol extract poroid fungus I. resulted in isolation citropremide (1), 3,4-dihydroxybenzalacetone (2) , lanosterol (3), ergost-6,8,22-trien-3β-ol (4), and ergosterol peroxide (5). The structures fungal compounds were determined on basis one- two-dimensional NMR MS spectroscopic analysis. Compounds 1–2 4–5 evaluated for...