New Dual Inhibitors of Tyrosyl-DNA Phosphodiesterase 1 and 2 Based on Deoxycholic Acid: Design, Synthesis, Cytotoxicity, and Molecular Modeling

New Dual Inhibitors of Tyrosyl-DNA Phosphodiesterase 1 and 2 Based on Deoxycholic Acid: Design, Synthesis, Cytotoxicity, and Molecular Modeling

Deoxycholic acid derivatives containing various heterocyclic functional groups at C-3 on the steroid scaffold were designed and synthesized as promising dual tyrosyl-DNA phosphodiesterase 1 and 2 (TDP1 and TDP2) inhibitors, which are potential targets to potentiate topoisomerase poison antitumor the...

Full description

Bibliographic Details
Main Authors:	Oksana V. Salomatina, Tatyana E. Kornienko, Alexandra L. Zakharenko, Nina I. Komarova, Chigozie Achara, Jóhannes Reynisson, Nariman F. Salakhutdinov, Olga I. Lavrik, Konstantin P. Volcho
Format:	Article
Language:	English
Published:	MDPI AG 2024-01-01
Series:	Molecules
Subjects:	deoxycholic acid oxirane thiols TDP1 inhibitor TDP2 inhibitor cancer
Online Access:	https://www.mdpi.com/1420-3049/29/3/581

Similar Items

New Deoxycholic Acid Derived Tyrosyl-DNA Phosphodiesterase 1 Inhibitors Also Inhibit Tyrosyl-DNA Phosphodiesterase 2
by: Oksana V. Salomatina, et al.
Published: (2021-12-01)

Novel Semisynthetic Derivatives of Bile Acids as Effective Tyrosyl-DNA Phosphodiesterase 1 Inhibitors
by: Oksana V. Salomatina, et al.
Published: (2018-03-01)

New Hybrid Compounds Combining Fragments of Usnic Acid and Monoterpenoids for Effective Tyrosyl-DNA Phosphodiesterase 1 Inhibition
by: Nadezhda S. Dyrkheeva, et al.
Published: (2021-07-01)

Synthesis of Norabietyl and Nordehydroabietyl Imidazolidine-2,4,5-Triones and Their Activity against Tyrosyl-DNA Phosphodiesterase 1
by: Kseniya S. Kovaleva, et al.
Published: (2023-11-01)

Novel group of tyrosyl-DNA-phosphodiesterase 1 inhibitors based on disaccharide nucleosides as drug prototypes for anti-cancer therapy
by: Anastasia O. Komarova, et al.
Published: (2018-01-01)

Discovery of Novel Sultone Fused Berberine Derivatives as Promising Tdp1 Inhibitors
by: Elizaveta D. Gladkova, et al.
Published: (2021-03-01)

Inhibition of Tyrosyl-DNA Phosphodiesterase 1 by Lipophilic Pyrimidine Nucleosides
by: Alexandra L. Zakharenko, et al.
Published: (2020-08-01)

Design, Synthesis, and Molecular Docking Study of New Tyrosyl-DNA Phosphodiesterase 1 (TDP1) Inhibitors Combining Resin Acids and Adamantane Moieties
by: Kseniya Kovaleva, et al.
Published: (2021-05-01)

Tdp1 Inhibition as a Promising Approach to New Anticancer Drugs
by: Konstantin Volcho, et al.
Published: (2019-08-01)

Sulfide, Sulfoxide, and Sulfone Derivatives of Usnic Acid as Inhibitors of Human TDP1 and TDP2 Enzymes
by: Aleksandr S. Filimonov, et al.
Published: (2024-12-01)

Adamantane-Monoterpenoid Conjugates Linked via Heterocyclic Linkers Enhance the Cytotoxic Effect of Topotecan
by: Aldar A. Munkuev, et al.
Published: (2022-05-01)

In Vitro and In Silico Studies of Human Tyrosyl-DNA Phosphodiesterase 1 (Tdp1) Inhibition by Stereoisomeric Forms of Lipophilic Nucleosides: The Role of Carbohydrate Stereochemistry in Ligand-Enzyme Interactions
by: Nadezhda S. Dyrkheeva, et al.
Published: (2022-04-01)

Novel Derivatives of Deoxycholic Acid Bearing Linear Aliphatic Diamine and Aminoalcohol Moieties and their Cyclic Analogs at the C3 Position: Synthesis and Evaluation of Their In Vitro Antitumor Potential
by: Andrey V. Markov, et al.
Published: (2019-07-01)

Tyrosyl-DNA phosphodiesterase 2 (Tdp2) repairs DNA-protein crosslinks and protects against double strand breaks in vivo
by: Ivan Anticevic, et al.
Published: (2024-08-01)

Eficiência energética de um trator agrícola utilizando duas configurações de tomada de potência
by: Ulisses Giacomini Frantz, et al.
Published: (2014-07-01)

Topoisomerase-Mediated DNA Damage in Neurological Disorders
by: Morgan Crewe, et al.
Published: (2021-11-01)

The Lipophilic Purine Nucleoside—Tdp1 Inhibitor—Enhances DNA Damage Induced by Topotecan In Vitro and Potentiates the Antitumor Effect of Topotecan In Vivo
by: Irina A. Chernyshova, et al.
Published: (2022-12-01)

Prion-like Spreading of Disease in TDP-43 Proteinopathies
by: Emma Pongrácová, et al.
Published: (2024-11-01)

SC75741, A Novel c-Abl Inhibitor, Promotes the Clearance of TDP25 Aggregates via ATG5-Dependent Autophagy Pathway
by: Dongheng Zhou, et al.
Published: (2021-10-01)

ALS-linked TDP-43M337V knock-in mice exhibit splicing deregulation without neurodegeneration
by: Seiji Watanabe, et al.
Published: (2020-01-01)

Increasing Brain Permeability of PHA-767491, a Cell Division Cycle 7 Kinase Inhibitor, with Biodegradable Polymeric Nanoparticles
by: Elisa Rojas-Prats, et al.
Published: (2021-01-01)

TDP-43 and Phosphorylated TDP-43 Levels in Paired Plasma and CSF Samples in Amyotrophic Lateral Sclerosis
by: Yuting Ren, et al.
Published: (2021-06-01)

DNA–protein cross-link repair: what do we know now?
by: Huimin Zhang, et al.
Published: (2020-01-01)

TTBK1 and CK1 inhibitors restore TDP-43 pathology and avoid disease propagation in lymphoblast from Alzheimer’s disease patients
by: Loreto Martinez-Gonzalez, et al.
Published: (2023-08-01)

TDP-43-M323K causes abnormal brain development and progressive cognitive and motor deficits associated with mislocalised and increased levels of TDP-43
by: Juan M. Godoy-Corchuelo, et al.
Published: (2024-04-01)

Optogenetic TDP-43 nucleation induces persistent insoluble species and progressive motor dysfunction in vivo
by: Charlton G. Otte, et al.
Published: (2020-12-01)

Tar DNA-binding protein-43 (TDP-43) regulates axon growth in vitro and in vivo
by: Vineeta Bhasker Tripathi, et al.
Published: (2014-05-01)

Design, Synthesis, and Biological Investigation of Novel Classes of 3-Carene-Derived Potent Inhibitors of TDP1
by: Irina V. Il’ina, et al.
Published: (2020-07-01)

Impact of Mesotherapy with Sodium Deoxycholate on Liver: Metabolic- and Sex-Specific Insights in Swiss mice
by: LEIDYANNE F. GONÇALVES, et al.
Published: (2025-02-01)

New Hydrazinothiazole Derivatives of Usnic Acid as Potent Tdp1 Inhibitors
by: Aleksander S. Filimonov, et al.
Published: (2019-10-01)

The Role of TAR DNA Binding Protein 43 (TDP-43) as a CandiDate Biomarker of Amyotrophic Lateral Sclerosis: A Systematic Review and Meta-Analysis
by: Caterina Maria Gambino, et al.
Published: (2023-01-01)

TDP-43 Pathology in Alzheimer’s Disease
by: Axel Meneses, et al.
Published: (2021-12-01)

The Development of Tyrosyl-DNA Phosphodiesterase 1 Inhibitors. Combination of Monoterpene and Adamantine Moieties via Amide or Thioamide Bridges
by: Arina A. Chepanova, et al.
Published: (2019-07-01)

Open-access database of literature derived drug-related Torsade de Pointes cases
by: Krumpholz Laura, et al.
Published: (2022-01-01)

Patterns of synaptic loss in human amyotrophic lateral sclerosis spinal cord: a clinicopathological study
by: Oumayma Aousji, et al.
Published: (2023-07-01)

Mechanisms of Neurosyphilis-Induced Dementia: Insights into Pathophysiology
by: Aya Fadel, et al.
Published: (2024-12-01)

Alternative 3′ UTR polyadenylation is disrupted in the rNLS8 mouse model of ALS/FTLD
by: Randall J. Eck, et al.
Published: (2025-01-01)

Novel in vivo TDP-43 stress reporter models to accelerate drug development in ALS
by: Febe Ferro, et al.
Published: (2024-10-01)

Effect of icaritin on autophagy-related protein expression in TDP-43-transfected SH-SY5Y cells
by: Yanjun Zhou, et al.
Published: (2022-07-01)

Sex Hormone-Binding Globulin (SHBG) in Cerebrospinal Fluid Does Not Discriminate between the Main FTLD Pathological Subtypes but Correlates with Cognitive Decline in FTLD Tauopathies
by: Marta del Campo, et al.
Published: (2021-10-01)