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Johannes Reynisson's Outputs (122)

Novel Semisynthetic Derivatives of Bile Acids as Effective Tyrosyl-DNA Phosphodiesterase 1 Inhibitors. (2018)
Journal Article
Reynisson. (2018). Novel Semisynthetic Derivatives of Bile Acids as Effective Tyrosyl-DNA Phosphodiesterase 1 Inhibitors. Molecules, https://doi.org/10.3390/molecules23030679

An Important task in the treatment of oncological and neurodegenerative diseases is the search for new inhibitors of DNA repair system enzymes. Tyrosyl-DNA phosphodiesterase 1 (Tdp1) is one of the DNA repair system enzymes involved in the removal of... Read More about Novel Semisynthetic Derivatives of Bile Acids as Effective Tyrosyl-DNA Phosphodiesterase 1 Inhibitors..

Aminoadamantanes containing monoterpene-derived fragments as potent tyrosyl-DNA phosphodiesterase 1 inhibitors (2018)
Journal Article
Ponomarev, K. Y., Suslov, E. V., Zakharenko, A. L., Zakharova, O. D., Rogachev, A. D., Korchagina, D. V., Zafar, A., Reynisson, J., Nefedov, A. A., Volcho, K. P., Salakhutdinov, N. F., & Lavrik, O. I. (2018). Aminoadamantanes containing monoterpene-derived fragments as potent tyrosyl-DNA phosphodiesterase 1 inhibitors. Bioorganic Chemistry, 76, 392-399. https://doi.org/10.1016/j.bioorg.2017.12.005

Investigation into Improving the Aqueous Solubility of the Thieno[2,3-b]pyridine Anti-Proliferative Agents (2018)
Journal Article
Reynisson, J. (2018). Investigation into Improving the Aqueous Solubility of the Thieno[2,3-b]pyridine Anti-Proliferative Agents. Molecules, https://doi.org/10.3390/molecules23010145

It is now established that the thieno[2,3-b]pyridines are a potent class of antiproliferatives. One of the main issues encountered for their clinical application is their low water solubility. In order to improve this, two strategies were pursued. Fi... Read More about Investigation into Improving the Aqueous Solubility of the Thieno[2,3-b]pyridine Anti-Proliferative Agents.

Thieno[2,3-b]pyridine derivatives are potent anti-platelet drugs, inhibiting platelet activation, aggregation and showing synergy with aspirin. (2018)
Journal Article
Reynisson. (2018). Thieno[2,3-b]pyridine derivatives are potent anti-platelet drugs, inhibiting platelet activation, aggregation and showing synergy with aspirin. European Journal of Medicinal Chemistry, 1997 - 2004. https://doi.org/10.1016/j.ejmech.2017.11.014

Drugs which inhibit platelet function are commonly used to prevent blood clot formation in patients with Acute Coronary Syndromes (ACS) or those at risk of stroke. The thieno[3,2-c]pyridine class of therapeutic agents, of which clopidogrel is the mos... Read More about Thieno[2,3-b]pyridine derivatives are potent anti-platelet drugs, inhibiting platelet activation, aggregation and showing synergy with aspirin..

GPCR Modulation of Thieno[2,3-b]pyridine Anti-Proliferative Agents. (2017)
Journal Article
Reynisson. (2017). GPCR Modulation of Thieno[2,3-b]pyridine Anti-Proliferative Agents. Molecules, https://doi.org/10.3390/molecules22122254

A panel of docking scaffolds was developed for the known molecular targets of the anticancer agents, thieno[2,3-b]pyridines, in order to glean insight into their mechanism of action. The reported targets are the copper-trafficking antioxidant 1 prote... Read More about GPCR Modulation of Thieno[2,3-b]pyridine Anti-Proliferative Agents..

Development and Application of an NMR-Based Assay for Polyphenol Oxidases (2017)
Journal Article
Li, Y., Zafar, A., Kilmartin, P. A., Reynisson, J., & Leung, I. K. H. (2017). Development and Application of an NMR-Based Assay for Polyphenol Oxidases. ChemistrySelect, 2(32), 10435-10441. https://doi.org/10.1002/slct.201702144

Polyphenol oxidases (PPOs) are enzymes that catalyse the oxidation of phenolic compounds. We report a NMR-based assay that can be used as a screening and validation tool for PPO activity modulators, which was demonstrated using a series of PPO inhibi... Read More about Development and Application of an NMR-Based Assay for Polyphenol Oxidases.

Development of NMR and thermal shift assays for the evaluation of Mycobacterium tuberculosis isocitrate lyase inhibitors. (2017)
Journal Article
Reynisson. (2017). Development of NMR and thermal shift assays for the evaluation of Mycobacterium tuberculosis isocitrate lyase inhibitors. MedChemComm, 2155 - 2163. https://doi.org/10.1039/c7md00456g

The enzymes isocitrate lyase (ICL) isoforms 1 and 2 are essential for Mycobacterium tuberculosis survival within macrophages during latent tuberculosis (TB). As such, ICLs are attractive therapeutic targets for the treatment of tuberculosis. However,... Read More about Development of NMR and thermal shift assays for the evaluation of Mycobacterium tuberculosis isocitrate lyase inhibitors..

Synthesis and in vitro Biological Evaluation of Ferrocenyl Side-Chain-Functionalized Paclitaxel Derivatives (2017)
Journal Article
Plażuk, D., Wieczorek, A., Ciszewski, W. M., Kowalczyk, K., Błauż, A., Pawlędzio, S., Makal, A., Eurtivong, C., Arabshahi, H. J., Reynisson, J., Hartinger, C. G., & Rychlik, B. (2017). Synthesis and in vitro Biological Evaluation of Ferrocenyl Side-Chain-Functionalized Paclitaxel Derivatives. ChemMedChem, 12(22), 1882-1892. https://doi.org/10.1002/cmdc.201700576

Taxanes, including paclitaxel, are widely used in cancer therapy. In an attempt to overcome some of the disadvantages entailed with taxane chemotherapy, we devised the synthesis of ferrocenyl-functionalized paclitaxel derivatives and studied their bi... Read More about Synthesis and in vitro Biological Evaluation of Ferrocenyl Side-Chain-Functionalized Paclitaxel Derivatives.

Anti-influenza activity of diazaadamantanes combined with monoterpene moieties (2017)
Journal Article
Suslov, E., Zarubaev, V. V., Slita, A. V., Ponomarev, K., Korchagina, D., Ayine-Tora, D. M., Reynisson, J., Volcho, K., & Salakhutdinov, N. (2017). Anti-influenza activity of diazaadamantanes combined with monoterpene moieties. Bioorganic and Medicinal Chemistry Letters, 27(19), 4531-4535. https://doi.org/10.1016/j.bmcl.2017.08.062

The antiviral activity of several diaza-adamantanes containing monoterpenoid moieties against a rimantadine-resistant strain of the influenza A/Puerto Rico/8/34 (H1N1) virus was studied. Hetero-adamantanes containing monoterpene moieties at the amina... Read More about Anti-influenza activity of diazaadamantanes combined with monoterpene moieties.

Preparation and evaluation of PLGA nanoparticle-loaded biodegradable light-responsive injectable implants as a promising platform for intravitreal drug delivery (2017)
Journal Article
Bisht, R., Jaiswal, J. K., Oliver, V. F., Eurtivong, C., Reynisson, J., & Rupenthal, I. D. (2017). Preparation and evaluation of PLGA nanoparticle-loaded biodegradable light-responsive injectable implants as a promising platform for intravitreal drug delivery. Journal of Drug Delivery Science and Technology, 40, 142-156. https://doi.org/10.1016/j.jddst.2017.06.006

The present study reports on the development of a hybrid system by integrating poly(lactic-co-glycolic)acid nanoparticles (PLGA NPs) into light-responsive in-situ forming injectable implants (ISFIs) for minimally invasive and safe intravitreal peptid... Read More about Preparation and evaluation of PLGA nanoparticle-loaded biodegradable light-responsive injectable implants as a promising platform for intravitreal drug delivery.

New Anti-Seizure (Arylalkyl)azole Derivatives: Synthesis,In VivoandIn SilicoStudies: Anti-Seizure (Arylalkyl)azole Derivatives (2017)
Journal Article
Sari, S., Dalkara, S., Kaynak, F. B., Reynisson, J., Saraç, S., & Karakurt, A. (2017). New Anti-Seizure (Arylalkyl)azole Derivatives: Synthesis,In VivoandIn SilicoStudies: Anti-Seizure (Arylalkyl)azole Derivatives. Archiv der Pharmazie / Chemistry in Life Sciences, 350(6), Article e201700043. https://doi.org/10.1002/ardp.201700043

(Arylalkyl)azoles are a class of antiepileptic compounds including nafimidone, denzimol, and loreclezole (LRZ). Nafimidone and denzimol are thought to inhibit voltage-gated sodium channels (VGSCs) and enhance γ-aminobutyric acid (GABA)-mediated respo... Read More about New Anti-Seizure (Arylalkyl)azole Derivatives: Synthesis,In VivoandIn SilicoStudies: Anti-Seizure (Arylalkyl)azole Derivatives.

Glycophenotype of breast and prostate cancer stem cells treated with thieno[2,3-b]pyridine anticancer compound. (2017)
Journal Article
Reynisson. (2017). Glycophenotype of breast and prostate cancer stem cells treated with thieno[2,3-b]pyridine anticancer compound. Drug Design, Development and Therapy, 759 - 769. https://doi.org/10.2147/DDDT.S121122

Tumor progression may be driven by a small subpopulation of cancer stem cells (CSCs characterized by CD44+/CD24- phenotype). We investigated the influence of a newly developed thienopyridine anticancer compound (3-amino-5-oxo-N-naphthyl-5,6,7, 8-tetr... Read More about Glycophenotype of breast and prostate cancer stem cells treated with thieno[2,3-b]pyridine anticancer compound..

New Iminodiacetate–Thiosemicarbazone Hybrids and Their Copper(II) Complexes Are Potential Ribonucleotide Reductase R2 Inhibitors with High Antiproliferative Activity (2017)
Journal Article
Zaltariov, M. F., Hammerstad, M., Arabshahi, H. J., Jovanović, K., Richter, K. W., Cazacu, M., Shova, S., Balan, M., Andersen, N. H., Radulović, S., Reynisson, J., Andersson, K. K., & Arion, V. B. (2017). New Iminodiacetate–Thiosemicarbazone Hybrids and Their Copper(II) Complexes Are Potential Ribonucleotide Reductase R2 Inhibitors with High Antiproliferative Activity. Inorganic Chemistry, 56(6), 3532-3549. https://doi.org/10.1021/acs.inorgchem.6b03178

As ribonucleotide reductase (RNR) plays a crucial role in nucleic acid metabolism, it is an important target for anticancer therapy. The thiosemicarbazone Triapine is an efficient R2 inhibitor, which has entered ∼20 clinical trials. Thiosemicarbazone... Read More about New Iminodiacetate–Thiosemicarbazone Hybrids and Their Copper(II) Complexes Are Potential Ribonucleotide Reductase R2 Inhibitors with High Antiproliferative Activity.

Synthesis and antiproliferative activity of 2-chlorophenyl carboxamide thienopyridines (2016)
Journal Article
van Rensburg, M., Leung, E., Haverkate, N. A., Eurtivong, C., Pilkington, L. I., Reynisson, J., & Barker, D. (2017). Synthesis and antiproliferative activity of 2-chlorophenyl carboxamide thienopyridines. Bioorganic and Medicinal Chemistry Letters, 27(2), 135-138. https://doi.org/10.1016/j.bmcl.2016.12.009

3-Amino-2-arylcarboxamide-thieno[2,3-b]pyridines are a known class of antiproliferative compounds with activity against the phospholipase C enzyme. To further investigate the structure activity relationships of these derivatives a series of analogues... Read More about Synthesis and antiproliferative activity of 2-chlorophenyl carboxamide thienopyridines.

3-Amino-thieno[2,3-b]pyridines as microtubule-destabilising agents: Molecular modelling and biological evaluation in the sea urchin embryo and human cancer cells (2016)
Journal Article
Eurtivong, C., Semenov, V., Semenova, M., Konyushkin, L., Atamanenko, O., Reynisson, J., & Kiselyov, A. (2017). 3-Amino-thieno[2,3-b]pyridines as microtubule-destabilising agents: Molecular modelling and biological evaluation in the sea urchin embryo and human cancer cells. Bioorganic and Medicinal Chemistry, 25(2), 658-664. https://doi.org/10.1016/j.bmc.2016.11.041

A series of 3-amino-thieno[2,3-b]pyridines was prepared and tested in a phenotypic sea urchin embryo assay to identify potent and specific molecules that affect tubulin dynamics. The most active compounds featured a tricyclic core ring system with a... Read More about 3-Amino-thieno[2,3-b]pyridines as microtubule-destabilising agents: Molecular modelling and biological evaluation in the sea urchin embryo and human cancer cells.

Coumarin Antifungal Lead Compounds from Millettia thonningii and Their Predicted Mechanism of Action (2016)
Journal Article
Reynisson. (2016). Coumarin Antifungal Lead Compounds from Millettia thonningii and Their Predicted Mechanism of Action. Molecules, https://doi.org/10.3390/molecules21101369

Fungal pathogens continue to pose challenges to humans and plants despite efforts to control them. Two coumarins, robustic acid and thonningine-C isolated from Millettia thonningii, show promising activity against the fungus Candida albicans with min... Read More about Coumarin Antifungal Lead Compounds from Millettia thonningii and Their Predicted Mechanism of Action.

Synthesis of 3-Amino-2-carboxamide Tetrahydropyrrolo[2,3-b]quinolines (2016)
Journal Article
Barker, D., Pilkington, L., Haverkate, N., van Rensburg, M., Reynisson, J., & Leung, E. (in press). Synthesis of 3-Amino-2-carboxamide Tetrahydropyrrolo[2,3-b]quinolines. SYNLETT, 27(20), 2811-2814. https://doi.org/10.1055/s-0036-1588619

This article communicates the first synthesis of 3-amino-2-carboxamide pyrrolo[2,3-b]quinolines and fused-ring pyrrolopyridines in an efficient synthesis via a Thorpe–Ziegler transformation. The reported synthetic route allows for a wide range of nit... Read More about Synthesis of 3-Amino-2-carboxamide Tetrahydropyrrolo[2,3-b]quinolines.

New inhibitors of tyrosyl-DNA phosphodiesterase I (Tdp 1) combining 7-hydroxycoumarin and monoterpenoid moieties (2016)
Journal Article
Khomenko, T., Zakharenko, A., Odarchenko, T., Arabshahi, H. J., Sannikova, V., Zakharova, O., Korchagina, D., Reynisson, J., Volcho, K., Salakhutdinov, N., & Lavrik, O. (2016). New inhibitors of tyrosyl-DNA phosphodiesterase I (Tdp 1) combining 7-hydroxycoumarin and monoterpenoid moieties. Bioorganic and Medicinal Chemistry, 24(21), 5573-5581. https://doi.org/10.1016/j.bmc.2016.09.016

A number of derivatives of 7-hydroxycoumarins containing aromatic or monoterpene substituents at hydroxy-group were synthesized based on a hit compound from a virtual screen. The ability of these compounds to inhibit tyrosyl-DNA phosphodiesterase I (... Read More about New inhibitors of tyrosyl-DNA phosphodiesterase I (Tdp 1) combining 7-hydroxycoumarin and monoterpenoid moieties.

Radical Chemistry and Cytotoxicity of Bioreductive 3-Substituted Quinoxaline Di-N-Oxides (2016)
Journal Article
Anderson, R. F., Yadav, P., Shinde, S. S., Hong, C. R., Pullen, S. M., Reynisson, J., Wilson, W. R., & Hay, M. P. (2016). Radical Chemistry and Cytotoxicity of Bioreductive 3-Substituted Quinoxaline Di-N-Oxides. Chemical Research in Toxicology, 29(8), 1310-1324. https://doi.org/10.1021/acs.chemrestox.6b00133

The radical chemistry and cytotoxicity of a series of quinoxaline di-N-oxide (QDO) compounds has been investigated to explore the mechanism of action of this class of bioreductive drugs. A series of water-soluble 3-trifluoromethyl (4–10), 3-phenyl (1... Read More about Radical Chemistry and Cytotoxicity of Bioreductive 3-Substituted Quinoxaline Di-N-Oxides.