Sesquiterpene Lactones Modulated DNA Methylation through Inhibition of DNMTs in Ovarian Cancer Cells (2022)
Journal Article
Kitchen, Li, & Reynisson. (2022). Sesquiterpene Lactones Modulated DNA Methylation through Inhibition of DNMTs in Ovarian Cancer Cells. https://doi.org/10.1016/j.prmcm.2022.100074

Inappropriate DNA methylation of tumour suppressor genes can affect their expression and function, and as such, DNA methylation has been a promising target for anti-cancer therapy. In gynaecological malignancy, ovarian cancer has the highest associat... Read More about Sesquiterpene Lactones Modulated DNA Methylation through Inhibition of DNMTs in Ovarian Cancer Cells.

Highly Antiproliferative Latonduine and Indolo[2,3-c]quinoline Derivatives: Complex Formation with Copper(II) Markedly Changes the Kinase Inhibitory Profile. (2022)
Journal Article
Reynisson. (2022). Highly Antiproliferative Latonduine and Indolo[2,3-c]quinoline Derivatives: Complex Formation with Copper(II) Markedly Changes the Kinase Inhibitory Profile. Journal of Medicinal Chemistry, 2238 - 2261. https://doi.org/10.1021/acs.jmedchem.1c01740

A series of latonduine and indoloquinoline derivatives HL1-HL8 and their copper(II) complexes (1-8) were synthesized and comprehensively characterized. The structures of five compounds (HL6, [CuCl(L1)(DMF)]·DMF, [CuCl(L2)(CH3OH)], [CuCl(L3)]·0.5H2O,... Read More about Highly Antiproliferative Latonduine and Indolo[2,3-c]quinoline Derivatives: Complex Formation with Copper(II) Markedly Changes the Kinase Inhibitory Profile..

Conjugation of Palbociclib with MHI-148 Has an Increased Cytotoxic Effect for Breast Cancer Cells and an Altered Mechanism of Action. (2022)
Journal Article
Reynisson. (2022). Conjugation of Palbociclib with MHI-148 Has an Increased Cytotoxic Effect for Breast Cancer Cells and an Altered Mechanism of Action. Molecules, 1-14. https://doi.org/10.3390/molecules27030880

The CDK4/6 inhibitor palbociclib, combined with endocrine therapy, has been shown to be effective in postmenopausal women with estrogen receptor-positive, HER2-negative advanced or metastatic breast cancer. However, palbociclib is not as effective in... Read More about Conjugation of Palbociclib with MHI-148 Has an Increased Cytotoxic Effect for Breast Cancer Cells and an Altered Mechanism of Action..

Sweet targets: sugar nucleotide biosynthesis inhibitors. (2022)
Journal Article
Ahmadipour, S., Reynisson, J., Field, R. A., & Miller, G. J. (2022). Sweet targets: sugar nucleotide biosynthesis inhibitors. Future Medicinal Chemistry, 14(5), 295-298. https://doi.org/10.4155/fmc-2021-0286

'Editorial Material'

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.

New Hybrid Compounds Combining Fragments of Usnic Acid and Monoterpenoids for Effective Tyrosyl-DNA Phosphodiesterase 1 Inhibition. (2021)
Journal Article
Reynisson. (2021). New Hybrid Compounds Combining Fragments of Usnic Acid and Monoterpenoids for Effective Tyrosyl-DNA Phosphodiesterase 1 Inhibition. Biomolecules, https://doi.org/10.3390/biom11070973

Usnic acid (UA) is a secondary metabolite of lichens that exhibits a wide range of biological activities. Previously, we found that UA derivatives are effective inhibitors of tyrosyl-DNA phosphodiesterase 1 (TDP1). It can remove covalent complex DNA-... Read More about New Hybrid Compounds Combining Fragments of Usnic Acid and Monoterpenoids for Effective Tyrosyl-DNA Phosphodiesterase 1 Inhibition..

Validating TDP1 as an Inhibition Target for the Development of Chemosensitizers for Camptothecin-Based Chemotherapy Drugs. (2021)
Journal Article
Reynisson, J. (2021). Validating TDP1 as an Inhibition Target for the Development of Chemosensitizers for Camptothecin-Based Chemotherapy Drugs. Oncology and Therapy,

Cancer chemotherapy sensitizers hold the key to maximizing the potential of standard anticancer treatments. We have a long-standing interest in developing and validating inhibitors of the DNA repair enzyme tyrosyl-DNA phosphodiesterase 1 (TDP1) as ch... Read More about Validating TDP1 as an Inhibition Target for the Development of Chemosensitizers for Camptothecin-Based Chemotherapy Drugs..

Novel Tdp1 Inhibitors Based on Adamantane Connected with Monoterpene Moieties via Heterocyclic Fragments. (2021)
Journal Article
Reynisson. (2021). Novel Tdp1 Inhibitors Based on Adamantane Connected with Monoterpene Moieties via Heterocyclic Fragments. Molecules, 1-23. https://doi.org/10.3390/molecules26113128

Tyrosyl-DNA phosphodiesterase 1 (Tdp1) is a promising target for anticancer therapy due to its ability to counter the effects topoisomerase 1 (Top1) poison, such as topotecan, thus, decreasing their efficacy. Compounds containing adamantane and monot... Read More about Novel Tdp1 Inhibitors Based on Adamantane Connected with Monoterpene Moieties via Heterocyclic Fragments..

Improving the solubility of anti-proliferative thieno[2,3-b]quinoline-2-carboxamides. (2021)
Journal Article
Reynisson. (2021). Improving the solubility of anti-proliferative thieno[2,3-b]quinoline-2-carboxamides. Bioorganic and Medicinal Chemistry, 1- 10. https://doi.org/10.1016/j.bmc.2021.116092

Thieno[2,3-b]pyridines are a class of compounds known for their potent anti-proliferative activities against a range of human cancer cell lines. In this research, a number of strategies to generate analogues that have improved aqueous solubility whil... Read More about Improving the solubility of anti-proliferative thieno[2,3-b]quinoline-2-carboxamides..

Discovery of novel Hsp90 C-terminal domain inhibitors that disrupt co-chaperone binding. (2021)
Journal Article
Reynisson. (2021). Discovery of novel Hsp90 C-terminal domain inhibitors that disrupt co-chaperone binding. Bioorganic and Medicinal Chemistry Letters, https://doi.org/10.1016/j.bmcl.2021.127857

Heat shock protein 90 (Hsp90) is an essential molecular chaperone that performs vital stress-related and housekeeping functions in cells and is a current therapeutic target for diseases such as cancers. Particularly, the development of Hsp90 C-termin... Read More about Discovery of novel Hsp90 C-terminal domain inhibitors that disrupt co-chaperone binding..

The First Berberine-Based Inhibitors of Tyrosyl-DNA Phosphodiesterase 1 (Tdp1), an Important DNA Repair Enzyme. (2020)
Journal Article
Reynisson. (2020). The First Berberine-Based Inhibitors of Tyrosyl-DNA Phosphodiesterase 1 (Tdp1), an Important DNA Repair Enzyme. International Journal of Molecular Sciences, https://doi.org/10.3390/ijms21197162

A series of berberine and tetrahydroberberine sulfonate derivatives were prepared and tested against the tyrosyl-DNA phosphodiesterase 1 (Tdp1) DNA-repair enzyme. The berberine derivatives inhibit the Tdp1 enzyme in the low micromolar range; this is... Read More about The First Berberine-Based Inhibitors of Tyrosyl-DNA Phosphodiesterase 1 (Tdp1), an Important DNA Repair Enzyme..

Glycosphingolipid expression at breast cancer stem cells after novel thieno[2,3-b]pyridine anticancer compound treatment. (2020)
Journal Article
Reynisson. (2020). Glycosphingolipid expression at breast cancer stem cells after novel thieno[2,3-b]pyridine anticancer compound treatment. Scientific reports, 11876 - ?. https://doi.org/10.1038/s41598-020-68516-y

Glycosphingolipid expression differs between human breast cancer stem cells (CSC) and cancer non-stem cells (non-CSC). We performed studies of viability, type of cell death, cancer stem cell percent and glycosphingolipid expression on CSC and non-CSC... Read More about Glycosphingolipid expression at breast cancer stem cells after novel thieno[2,3-b]pyridine anticancer compound treatment..

Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes-7. (2020)
Journal Article
Reynisson. (2020). Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes-7. Molecules, https://doi.org/10.3390/molecules25132968

Breakthroughs in Medicinal Chemistry [...].

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..