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Indolo[2,3- e ]benzazocines and indolo[2,3- f ]benzazonines and their copper( ii ) complexes as microtubule destabilizing agents † (2023)
Journal Article
Wittmann, C., Dömötör, O., Kuznetcova, I., Spengler, G., Reynisson, J., Holder, L., …Arion, V. B. (2023). Indolo[2,3- e ]benzazocines and indolo[2,3- f ]benzazonines and their copper( ii ) complexes as microtubule destabilizing agents †. Dalton Transactions, 52(29), 9964-9982. https://doi.org/10.1039/d3dt01632c

A series of four indolo[2,3-e]benzazocines HL1–HL4 and two indolo[2,3-f]benzazonines HL5 and HL6, as well as their respective copper(ii) complexes 1–6, were synthesized and characterized by 1H and 13C NMR spectroscopy, ESI mass spectrometry, single c... Read More about Indolo[2,3- e ]benzazocines and indolo[2,3- f ]benzazonines and their copper( ii ) complexes as microtubule destabilizing agents †.

Impact of the ferrocenyl group on cytotoxicity and KSP inhibitory activity of ferrocenyl monastrol conjugates (2021)
Journal Article
Reynisson, J., Wieczorek-Błauż, A., Kowalczyk, K., Błauż, A., Makal, A., Pawlędzio, S., …Plażuk, D. (2021). Impact of the ferrocenyl group on cytotoxicity and KSP inhibitory activity of ferrocenyl monastrol conjugates. Dalton Transactions, 51(2), 491-508. https://doi.org/10.1039/d1dt03553c

The incorporation of the ferrocenyl moiety into a bioactive molecule may significantly alter the activity of the resulting conjugate. By applying this strategy, we designed ferrocenyl analogs of monastrol - the first low molecular weight kinesin spin... Read More about Impact of the ferrocenyl group on cytotoxicity and KSP inhibitory activity of ferrocenyl monastrol conjugates.

An optimised MALDI-TOF assay for phosphatidylcholine-specific phospholipase C. (2021)
Journal Article
Reynisson. (2021). An optimised MALDI-TOF assay for phosphatidylcholine-specific phospholipase C. Analytical Methods, https://doi.org/10.1039/D0AY02208J

The Bacillus cereus phosphatidylcholine-specific phospholipase C (PC-PLCBc) is an enzyme that catalyses the hydrolysis of phosphatidylcholines into phosphocholine and 1,2-diacylglycerols. PC-PLCBc has found applications in both the food industry and... Read More about An optimised MALDI-TOF assay for phosphatidylcholine-specific phospholipase C..

Metal-Dependent Cytotoxic and Kinesin Spindle Protein Inhibitory Activity of Ru, Os, Rh, and Ir Half-Sandwich Complexes of Ispinesib-Derived Ligands (2020)
Journal Article
Reynisson. (2020). Metal-Dependent Cytotoxic and Kinesin Spindle Protein Inhibitory Activity of Ru, Os, Rh, and Ir Half-Sandwich Complexes of Ispinesib-Derived Ligands. Inorganic Chemistry, 14879-14890. https://doi.org/10.1021/acs.inorgchem.0c00957

Ispinesib is a potent inhibitor of kinesin spindle protein (KSP), which has been identified as a promising target for antimitotic anticancer drugs. Herein, we report the synthesis of half-sandwich complexes of Ru, Os, Rh, and Ir bearing the ispinesib... Read More about Metal-Dependent Cytotoxic and Kinesin Spindle Protein Inhibitory Activity of Ru, Os, Rh, and Ir Half-Sandwich Complexes of Ispinesib-Derived Ligands.

Promising New Inhibitors of Tyrosyl-DNA Phosphodiesterase I (Tdp 1) Combining 4-Arylcoumarin and Monoterpenoid Moieties as Components of Complex Antitumor Therapy (2019)
Journal Article
Reynisson. (2019). Promising New Inhibitors of Tyrosyl-DNA Phosphodiesterase I (Tdp 1) Combining 4-Arylcoumarin and Monoterpenoid Moieties as Components of Complex Antitumor Therapy. International Journal of Molecular Sciences, https://doi.org/10.3390/ijms21010126

Tyrosyl-DNA phosphodiesterase 1 (Tdp1) is an important DNA repair enzyme in humans, and a current and promising inhibition target for the development of new chemosensitizing agents due to its ability to remove DNA damage caused by topoisomerase 1 (To... Read More about Promising New Inhibitors of Tyrosyl-DNA Phosphodiesterase I (Tdp 1) Combining 4-Arylcoumarin and Monoterpenoid Moieties as Components of Complex Antitumor Therapy.

Identification of novel inhibitors for the tyrosyl-DNA-phosphodiesterase 1 (Tdp1) mutant SCAN1 using virtual screening. (2019)
Journal Article
Reynisson. (2019). Identification of novel inhibitors for the tyrosyl-DNA-phosphodiesterase 1 (Tdp1) mutant SCAN1 using virtual screening. Bioorganic and Medicinal Chemistry, 115234 - ?. https://doi.org/10.1016/j.bmc.2019.115234

Spinocerebellar ataxia syndrome with axonal neuropathy (SCAN1) is a debilitating neurological disease that is caused by the mutation the Tyrosyl-DNA phosphodiesterase 1 (TDP1) DNA repair enzyme. The crucial His493 in TDP1's binding site is replaced w... Read More about Identification of novel inhibitors for the tyrosyl-DNA-phosphodiesterase 1 (Tdp1) mutant SCAN1 using virtual screening..

Identification of Isoform-Selective Ligands for the Middle Domain of Heat Shock Protein 90 (Hsp90) (2019)
Journal Article
Reynisson. (2019). Identification of Isoform-Selective Ligands for the Middle Domain of Heat Shock Protein 90 (Hsp90). International Journal of Molecular Sciences, https://doi.org/10.3390/ijms20215333

The molecular chaperone heat shock protein 90 (Hsp90) is a current inhibition target for the treatment of diseases, including cancer. In humans, there are two major cytosolic isoforms of Hsp90 (Hsp90a and Hsp90ß). Hsp90a is inducible and Hsp90ß is co... Read More about Identification of Isoform-Selective Ligands for the Middle Domain of Heat Shock Protein 90 (Hsp90).

New Hydrazinothiazole Derivatives of Usnic Acid as Potent Tdp1 Inhibitors. (2019)
Journal Article
Reynisson, J. (2019). New Hydrazinothiazole Derivatives of Usnic Acid as Potent Tdp1 Inhibitors. Molecules, https://doi.org/10.3390/molecules24203711

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 usni... Read More about New Hydrazinothiazole Derivatives of Usnic Acid as Potent Tdp1 Inhibitors..

New Water-Soluble Copper(II) Complexes with Morpholine-Thiosemicarbazone Hybrids: Insights into the Anticancer and Antibacterial Mode of Action. (2018)
Journal Article
Reynisson. (2018). New Water-Soluble Copper(II) Complexes with Morpholine-Thiosemicarbazone Hybrids: Insights into the Anticancer and Antibacterial Mode of Action. Journal of Medicinal Chemistry, https://doi.org/10.1021/acs.jmedchem.8b01031

Six morpholine-(iso)thiosemicarbazone hybrids HL1-HL6 and their Cu(II) complexes with good-to-moderate solubility and stability in water were synthesized and characterized. Cu(II) complexes [Cu(L1-6)Cl] (1-6) formed weak dimeric associates in the sol... Read More about New Water-Soluble Copper(II) Complexes with Morpholine-Thiosemicarbazone Hybrids: Insights into the Anticancer and Antibacterial Mode of Action..

A Novel Class of Tyrosyl-DNA Phosphodiesterase 1 Inhibitors That Contains the Octahydro-2H-chromen-4-ol Scaffold. (2018)
Journal Article
Li-Zhulanov, N. S., Zakharenko, A. L., Chepanova, A. A., Patel, J., Zafar, A., Volcho, K. P., …Lavrik, O. I. (2018). A Novel Class of Tyrosyl-DNA Phosphodiesterase 1 Inhibitors That Contains the Octahydro-2H-chromen-4-ol Scaffold. Molecules, 23(10), Article 2468. https://doi.org/10.3390/molecules23102468

Tyrosyl-DNA phosphodiesterase 1 (Tdp1) is a DNA repair enzyme that mends topoisomerase 1-mediated DNA damage. Tdp1 is a current inhibition target for the development of improved anticancer treatments, as its inhibition may enhance the therapeutic eff... Read More about A Novel Class of Tyrosyl-DNA Phosphodiesterase 1 Inhibitors That Contains the Octahydro-2H-chromen-4-ol Scaffold..

Synthesis, antibacterial, and antibiofilm potential of human autophagy 16 polypeptide and analogues (2018)
Journal Article
Reynisson. (2018). Synthesis, antibacterial, and antibiofilm potential of human autophagy 16 polypeptide and analogues. Peptide Science, e24076. https://doi.org/10.1002/pep2.24076

This work demonstrates that the human autophagy 16 polypeptide (Atg16) has antibacterial and antibiofilm potential, perturbs both Gram positive and negative bacterial membranes and subsequently also produces ROS in compromised bacteria. Engineered At... Read More about Synthesis, antibacterial, and antibiofilm potential of human autophagy 16 polypeptide and analogues.

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..

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 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..

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..

Evidence that phospholipase C is involved in the antitumour action of NSC768313, a new thieno[2,3-b]pyridine derivative. (2016)
Journal Article
Reynisson. (2016). Evidence that phospholipase C is involved in the antitumour action of NSC768313, a new thieno[2,3-b]pyridine derivative. Cancer cell international, 18 - ?. https://doi.org/10.1186/s12935-016-0293-6

BACKGROUND: The thieno[2,3-b]pyridines were discovered by virtual high throughput screening as potential inhibitors of phospholipase C (PLC) isoforms and showed potent growth inhibitory effects in National Cancer Institute's human tumour cell line pa... Read More about Evidence that phospholipase C is involved in the antitumour action of NSC768313, a new thieno[2,3-b]pyridine derivative..

Target profiling of an antimetastatic RAPTA agent by chemical proteomics: relevance to the mode of action. (2015)
Journal Article
Reynisson. (2015). Target profiling of an antimetastatic RAPTA agent by chemical proteomics: relevance to the mode of action. Chemical Science, 2449 - 2456. https://doi.org/10.1039/c4sc03905j

The clinical development of anticancer metallodrugs is often hindered by the elusive nature of their molecular targets. To identify the molecular targets of an antimetastatic ruthenium organometallic complex based on 1,3,5-triaza-7-phosphaadamantane... Read More about Target profiling of an antimetastatic RAPTA agent by chemical proteomics: relevance to the mode of action..