Search Results - "SZECSI, Mihály"
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Synthesis of regioisomeric 17β-N-phenylpyrazolyl steroid derivatives and their inhibitory effect on 17α-hydroxylase/C17,20-lyase
Published in Steroids (01-06-2010)“…The reaction of 3β-hydroxy-21-hydroxymethylidenepregn-5-en-3β-ol-20-one (1) with phenylhydrazine (2a) affords two regioisomers,…”
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Novel series of 17β-pyrazolylandrosta-5,16-diene derivatives and their inhibitory effect on 17α-hydroxylase/C17,20-lyase
Published in Steroids (01-09-2012)“…► Novel steroidal pyrazole regioisomers were synthesized. ► These compounds contain a double bond in position 16. ► The regioisomers were tested for their…”
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3
Steroselective synthesis of some steroidal oxazolines, as novel potential inhibitors of 17α-hydroxylase-C17,20-lyase
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4
Non-genomic actions of sex hormones on pregnant uterine contractility in rats: An in vitro study at term
Published in Life sciences (1973) (15-12-2020)“…The non-genomic (prompt) actions of sex steroids on pregnant uterine contractility are not fully explored yet, the aim of our study was to clarify such effects…”
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Non-genomic uterorelaxant actions of corticosteroid hormones in rats: An in vitro and in vivo study
Published in European journal of pharmacology (15-11-2022)“…We aimed to identify the short-term effects of a glucocorticoid (GC) and a mineralocorticoid (MC) on non-pregnant and late pregnant rat uterine contractions to…”
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Synthesis, Biological Evaluation and Docking Studies of 13-Epimeric 10-fluoro- and 10-Chloroestra-1,4-dien-3-ones as Potential Aromatase Inhibitors
Published in Molecules (Basel, Switzerland) (08-05-2019)“…Fluorination of 13-epimeric estrones and their 17-deoxy counterparts was performed with Selectfluor as the reagent. In acetonitrile or trifluoroacetic acid…”
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Synthesis of D-ring-substituted (5′R)- and (5′S)-17β-pyrazolinylandrostene epimers and comparison of their potential anticancer activities
Published in Steroids (01-04-2012)“…► Steroidal 17β-pyrazolines were prepared from 21-benzalpregnenolone derivatives. ► The reaction afforded a mixture of 5′R and 5′S pyrazolinylandrostene…”
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Synthesis of novel 13α-estrone derivatives by Sonogashira coupling as potential 17β-HSD1 inhibitors
Published in Beilstein journal of organic chemistry (30-06-2017)“…Novel 13α-estrone derivatives were synthesized by Sonogashira coupling. Transformations of 2- or 4-iodo regioisomers of 13α-estrone and its 3-methyl ether were…”
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9
Heterocyclic androstane and estrane d-ring modified steroids: Microwave-assisted synthesis, steroid-converting enzyme inhibition, apoptosis induction, and effects on genes encoding estrogen inactivating enzymes
Published in The Journal of steroid biochemistry and molecular biology (01-11-2021)“…[Display omitted] •d-ring–modified heterocyclic steroids are synthesized by microwave-assisted reactions.•d-ring–fused triazole estrone analog, compound 24,…”
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Synthesis and structure-activity relationships of 2- and/or 4-halogenated 13β- and 13α-estrone derivatives as enzyme inhibitors of estrogen biosynthesis
Published in Journal of enzyme inhibition and medicinal chemistry (01-01-2018)“…Ring A halogenated 13α-, 13β-, and 17-deoxy-13α-estrone derivatives were synthesised with N-halosuccinimides as electrophile triggers. Substitutions occurred…”
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Efficient access to novel androsteno-17-(1′,3′,4′)-oxadiazoles and 17β-(1′,3′,4′)-thiadiazoles via N-substituted hydrazone and N,N′-disubstituted hydrazine intermediates, and their pharmacological evaluation in vitro
Published in European journal of medicinal chemistry (15-06-2015)“…A series of novel 17-exo-oxadiazoles and -thiadiazoles in the Δ5 androstene series were efficiently synthesized from pregnenolone acetate and pregnadienolone…”
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Synthesis and Biological Evaluation of Triazolyl 13α-Estrone-Nucleoside Bioconjugates
Published in Molecules (Basel, Switzerland) (10-09-2016)“…2'-Deoxynucleoside conjugates of 13α-estrone were synthesized by applying the copper-catalyzed alkyne-azide click reaction (CuAAC). For the introduction of the…”
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13
Synthesis of substituted 15β-alkoxy estrone derivatives and their cofactor-dependent inhibitory effect on 17β-HSD1
Published in Journal of enzyme inhibition and medicinal chemistry (01-01-2019)“…17β-Hydroxysteroid dehydrogenase type 1 (17β-HSD1) is a key enzyme in the biosynthesis of 17β-estradiol. Novel estrone-based compounds bearing various…”
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14
Pd-Catalyzed microwave-assisted synthesis of phosphonated 13α-estrones as potential OATP2B1, 17β-HSD1 and/or STS inhibitors
Published in Beilstein journal of organic chemistry (14-11-2018)“…Novel 2- or 4-phosphonated 13α-estrone derivatives were synthesized via the Hirao reaction. Bromo regioisomers (2- or 4-) of 13α-estrone and its 3-benzyl or…”
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Synthesis and in vitro pharmacological evaluation of N-[(1-benzyl-1,2,3-triazol-4-yl)methyl]-carboxamides on d-secoestrone scaffolds
Published in Journal of enzyme inhibition and medicinal chemistry (03-07-2016)“…An efficient synthesis of several N-[(1-benzyl-1,2,3-triazol-4-yl)methyl]carboxamides in the 13β- and 13α-d-secoestrone series is reported. Novel triazoles…”
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Synthesis of A-ring halogenated 13α-estrone derivatives as potential 17β-HSD1 inhibitors
Published in Steroids (01-12-2015)“…[Display omitted] •13α-Estrone and some of its 3-ethers were subjected to aromatic halogenations.•The substituent on C-3 greatly affected the chemo- and the…”
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Synthesis of methoxycarbonylpyrazolylandrostene derivatives, and their potential inhibitory effect on androgen biosynthesis and cell proliferation
Published in Steroids (01-06-2015)“…[Display omitted] •Synthesis of 3-methoxycarbonyl-1-phenyl-5-pyrazolylandrostene derivatives.•Inhibition of the enzyme Δ5-3β-HSD by 17β-pyrazolylandrost-5-ene…”
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18
Antihormonal potential of selected D-homo and D-seco estratriene derivatives
Published in Steroids (01-05-2015)“…•New D-homo and 16,17-seco-estratriene compounds were synthesised and characterized.•Docking studies were performed for protein targets of steroidal…”
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Steroidal ferrocenes as potential enzyme inhibitors of the estrogen biosynthesis
Published in Biologia futura (01-09-2020)“…The potential inhibitory effect of diverse triazolyl-ferrocene steroids on key enzymes of the estrogen biosynthesis was investigated. Test compounds were…”
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Microwave assisted synthesis and biomedical potency of salicyloyloxy and 2-methoxybenzoyloxy androstane and stigmastane derivatives
Published in Steroids (01-02-2015)“…[Display omitted] •New steroidal salicyloyl esters were synthesized by MW and conventional methods.•Antioxidant and cytotoxic activity of new compounds was…”
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