Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes–5

Mangoni, Arduino A.; Eynde, Jean Jacques Vanden; Jampílek, Josef; Hadjipavlou‐Litina, Dimitra; Hong, Liu; Reynisson, Jóhannes; Sousa, Emı́lia; Gomes, Paula; Prókai-Tátrai, Katalin; Tuccinardi, Tiziano; Sabatier, Jean‐Marc; Luque, F. Javier; Rautio, Jarkko; Vasconcelos, M. Helena; Gemma, Sandra; Galdiero, Stefania; Hulme, Christopher; Collina, Simona; Gütschow, Michael; Kokotos, George; Siciliano, Carlo; Capasso, Raffaele; Agrofoglio, Luigi A.; Ragno, Rino; Muñoz‐Torrero, Diego

doi:10.3390/molecules24132415

Cited by 4 publications

(2 citation statements)

References 41 publications

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“…The use of DNA repair enzyme inhibitors as an adjuvant therapy to treat oncological disorders is one of the breakthroughs in modern cancer therapies [1,2]. Inhibition of DNA repair enzymes increases the effectiveness of chemotherapy drugs, especially for drug-resistant tumors.…”

Section: Introductionmentioning

confidence: 99%

New Hydrazinothiazole Derivatives of Usnic Acid as Potent Tdp1 Inhibitors

et al. 2019

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Tyrosyl-DNA phosphodiesterase 1 (Tdp1) is a promising therapeutic target in cancer therapy. Combination chemotherapy using Tdp1 inhibitors as a component can potentially improve therapeutic response to many chemotherapeutic regimes. A new set of usnic acid derivatives with hydrazonothiazole pharmacophore moieties were synthesized and evaluated as Tdp1 inhibitors. Most of these compounds were found to be potent inhibitors with IC50 values in the low nanomolar range. The activity of the compounds was verified by binding experiments and supported by molecular modeling. The ability of the most effective inhibitors, used at non-toxic concentrations, to sensitize tumors to the anticancer drug topotecan was also demonstrated. The order of administration of the inhibitor and topotecan on their synergistic effect was studied, suggesting that prior or simultaneous introduction of the inhibitor with topotecan is the most effective.

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Section: Introductionmentioning

confidence: 99%

New Hydrazinothiazole Derivatives of Usnic Acid as Potent Tdp1 Inhibitors

et al. 2019

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“…Moreover, atrasentan has shown some adverse effects, such as fluid retention and an increased risk of hospitalization for heart failure [11]. Advancement in molecular biology has provided important techniques that play a pivotal role in the modern drug development process [12], allowing the discovery of several new drug targets, especially in oncology [13][14][15][16][17][18]. On the other hand, drug repurposing is becoming a more and more attractive approach among pharmaceutical companies due to the clear advantages in cost and time reduction compared to de novo drug development [19,20].…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Molecular Modelling Studies of New 1,3-Diaryl-5-Oxo-Proline Derivatives as Endothelin Receptor Ligands

et al. 2020

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The synthesis of seventeen new 1,3-diaryl-5-oxo-proline derivatives as endothelin receptor (ETR) ligands is described. The structural configuration of the new molecules was determined by analyzing selected signals in proton NMR spectra. In vitro binding assays of the human ETA and ETB receptors allowed us to identify compound 31h as a selective ETAR ligand. The molecular docking of the selected compounds and the ETA antagonist atrasentan in the ETAR homology model provided insight into the structural elements required for the affinity and the selectivity of the ETAR subtype.

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Synthesis, in vitro evaluation and molecular docking studies of novel naphthoisoxazolequinone carboxamide hybrids as potential antitumor agents

Maldonado

Acevedo

Molinari

et al. 2022

Polycyclic Aromatic Compounds

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Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes–5

Abstract: Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes is a series of Editorials which is published on a biannual basis by the Editorial Board of the Medicinal Chemistry section of the journal Molecules [...]

Cited by 4 publications

References 41 publications

New Hydrazinothiazole Derivatives of Usnic Acid as Potent Tdp1 Inhibitors

New Hydrazinothiazole Derivatives of Usnic Acid as Potent Tdp1 Inhibitors

Synthesis and Molecular Modelling Studies of New 1,3-Diaryl-5-Oxo-Proline Derivatives as Endothelin Receptor Ligands

Synthesis, in vitro evaluation and molecular docking studies of novel naphthoisoxazolequinone carboxamide hybrids as potential antitumor agents

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