Search Results - "Gurská, Soňa"
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1
Metallacarborane Sulfamides: Unconventional, Specific, and Highly Selective Inhibitors of Carbonic Anhydrase IX
Published in Journal of medicinal chemistry (14-11-2019)“…Carbonic anhydrase IX (CAIX) is a transmembrane enzyme that regulates pH in hypoxic tumors and promotes tumor cell survival. Its expression is associated with…”
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2
Synthesis of Polycyclic Hetero-Fused 7‑Deazapurine Heterocycles and Nucleosides through C–H Dibenzothiophenation and Negishi Coupling
Published in Journal of the American Chemical Society (26-10-2022)“…A new approach for synthesizing polycyclic heterofused 7-deazapurine heterocycles and the corresponding nucleosides was developed based on C–H…”
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3
Synthesis and Cytostatic and Antiviral Profiling of Thieno-Fused 7‑Deazapurine Ribonucleosides
Published in Journal of medicinal chemistry (23-03-2017)“…Two isomeric series of new thieno-fused 7-deazapurine ribonucleosides (derived from 4-substituted thieno[2′,3′:4,5]pyrrolo[2,3-d]pyrimidines and…”
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4
Mixture Effects of Tryptophan Intestinal Microbial Metabolites on Aryl Hydrocarbon Receptor Activity
Published in International journal of molecular sciences (16-09-2022)“…Aryl hydrocarbon receptor (AHR) plays pivotal roles in intestinal physiology and pathophysiology. Intestinal AHR is activated by numerous dietary, endogenous,…”
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5
Synthesis and biological evaluation of triterpenoid thiazoles derived from betulonic acid, dihydrobetulonic acid, and ursonic acid
Published in European journal of medicinal chemistry (01-01-2020)“…In this work, 35 new derivatives of betulonic, dihydrobetulonic and ursonic acid were prepared including 30 aminothiazoles and all of them were tested for…”
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6
AminoBODIPY Conjugates for Targeted Drug Delivery Systems and Real-Time Monitoring of Drug Release
Published in Molecular pharmaceutics (07-06-2021)“…In this work, we report two concepts of drug delivery based on small-molecule drug conjugates with the ability of specific targeting and drug release…”
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7
Synthesis and Biological Profiling of Pyrazolo-Fused 7‑Deazapurine Nucleosides
Published in Journal of organic chemistry (21-08-2020)“…A series of 8-substituted 1-methyl-1,4-dihydropyrazolo[3′,4′:4,5]pyrrolo[2,3-d]pyrimidine (methylpyrazolo-fused 7-deazapurine) ribonucleosides have been…”
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8
Synthesis and Cytotoxic and Antiviral Profiling of Pyrrolo- and Furo-Fused 7‑Deazapurine Ribonucleosides
Published in Journal of medicinal chemistry (25-10-2018)“…Three series of isomeric pyrrolo- and furo-fused 7-deazapurine ribonucleosides were synthesized and screened for cytostatic and antiviral activity. The…”
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9
Click estradiol dimers with novel aromatic bridging units: synthesis and anticancer evaluation
Published in Journal of enzyme inhibition and medicinal chemistry (01-12-2024)“…Estradiol dimers (EDs) possess significant anticancer activity by targeting tubulin dynamics. In this study, we synthesised 12 EDs variants via…”
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10
Synthesis and Biological Evaluation of Oxindole Sulfonamide Derivatives as Bruton's Tyrosine Kinase Inhibitors
Published in ChemMedChem (02-01-2024)“…Bruton's tyrosine kinase (BTK) is a promising molecular target for several human B‐cell‐related autoimmune disorders, inflammation, and haematological…”
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11
Novel triterpenoid pyrones, phthalimides and phthalates are selectively cytotoxic in CCRF-CEM cancer cells – Synthesis, potency, and mitochondrial mechanism of action
Published in European journal of medicinal chemistry (05-04-2024)“…A series of triterpenoid pyrones was synthesized and subsequently modified to introduce phthalimide or phthalate moieties into the triterpenoid skeleton. These…”
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12
Synthesis and Biological Profiling of Benzofuro‐Fused 7‐Deazapurine Nucleosides
Published in European journal of organic chemistry (21-11-2023)“…A series of benzofuro‐fused 7‐deazapurine (6H‐furo[2,3‐e]pyrimido[4,5‐b]indole) 2’‐deoxyribo‐ and ribonucleosides was designed and synthesized. The synthesis…”
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13
Synthesis, Photophysical Properties, and Biological Profiling of Benzothieno-Fused 7-Deazapurine Ribonucleosides
Published in Journal of organic chemistry (19-06-2020)“…Two isomeric series of benzothieno-fused 7-deazapurine (benzo[4',5']thieno[3',2':4,5]- and benzo[4',5']thieno[2',3':4,5]pyrrolo[2,3- ]pyrimidine)…”
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14
Synthesis and Biological Profiling of Quinolino-Fused 7‑Deazapurine Nucleosides
Published in ACS omega (07-05-2024)“…A series of quinolino-fused 7-deazapurine (pyrimido[5′,4′:4,5]pyrrolo[3,2-f]quinoline) ribonucleosides were designed and synthesized. The synthesis of the…”
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15
Lupane derivatives containing various aryl substituents in the position 3 have selective cytostatic effect in leukemic cancer cells including resistant phenotypes
Published in European journal of medicinal chemistry (15-12-2022)“…In this work, a large set of betulinic acid derivatives modified with various aromatic substituents at the position C-3 were prepared via Suzuki-Myiaura…”
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16
Estradiol dimer inhibits tubulin polymerization and microtubule dynamics
Published in The Journal of steroid biochemistry and molecular biology (01-10-2018)“…[Display omitted] •Estradiol dimer inhibits tubulin assembly in vitro.•Estradiol dimer reversibly disrupts microtubule structures in U2OS cells.•Estradiol…”
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17
Novel 5‑Substituted Oxindole Derivatives as Bruton’s Tyrosine Kinase Inhibitors: Design, Synthesis, Docking, Molecular Dynamics Simulation, and Biological Evaluation
Published in ACS omega (20-02-2024)“…Bruton’s tyrosine kinase (BTK) is a non-RTK cytoplasmic kinase predominantly expressed by hemopoietic lineages, particularly B-cells. A new oxindole-based…”
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18
C‐5 Aryl Substituted Azaspirooxindolinones Derivatives: Synthesis and Biological Evaluation as Potential Inhibitors of Tec Family Kinases
Published in European journal of organic chemistry (07-09-2021)“…The interleukin‐2‐inducible kinase (ITK) and Bruton tyrosine kinase (BTK) are two crucial Tec family kinase members with important roles in the development of…”
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19
Substituted dienes prepared from betulinic acid – Synthesis, cytotoxicity, mechanism of action, and pharmacological parameters
Published in European journal of medicinal chemistry (15-11-2021)“…A set of new substituted dienes were synthesized from betulinic acid by its oxidation to 30-oxobetulinic acid followed by the Wittig reaction. Cytotoxicity of…”
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20
Synthesis, Leishmanicidal, Trypanocidal, Antiproliferative Assay and Apoptotic Induction of (2-Phenoxypyridin-3-yl)naphthalene-1(2 H )-one Derivatives
Published in Molecules (Basel, Switzerland) (31-08-2022)“…The coexistence of leishmaniasis, Chagas disease, and neoplasia in endemic areas has been extensively documented. The use of common drugs in the treatment of…”
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