Projects funded by the NCN

Information on the principal investigator and host institution

Information of the project and the call

Keywords

Equipment

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Thymol-derived 1,3,5-triazines, the non-indole and non-sulfone 5-HT6 receptor ligands, as a starter in search for an innovative treatment of memory- and mood disorders

2018/31/B/NZ7/02160

Keywords:

serotonin 5-HT6 triazine thymol selenium procognitive depression

Descriptors:

  • NZ7_14: Pharmacy, pharmacotherapy, pharmacology
  • ST5_16:

Panel:

NZ7 - Diagnostic tools, therapies and public health: public health, epidemiology, environmental health risks and occupational medicine, medical ethics, drug discovery and therapies, pharmacology

Host institution :

Uniwersytet Jagielloński – Collegium Medicum, Collegium Medicum, Wydział Farmaceutyczny

woj. małopolskie

Other projects carried out by the institution 

Principal investigator (from the host institution):

prof. Jadwiga Handzlik 

Number of co-investigators in the project: 12

Call: OPUS 16 - announced on 2018-09-14

Amount awarded: 1 997 976 PLN

Project start date (Y-m-d): 2019-07-26

Project end date (Y-m-d): 2023-07-25

Project duration:: 48 months (the same as in the proposal)

Project status: Project settled

Project description

Download the project description in a pdf file

Note - project descriptions were prepared by the authors of the applications themselves and placed in the system in an unchanged form.

Equipment purchased [PL]

  1. Liofilizator z pompą próżniową (70 000 PLN)
  2. Homogenizator (11 992 PLN)
  3. Używany aparat HPLC z detektorem UV-Vis i gwarancją serwisu (55 000 PLN)
  4. Wyparka rotacyjna z systemem próżniowym (35 000 PLN)

Information in the final report

  • Publication in academic press/journals (13)
  1. Chemical update on the potential for serotonin 5-HT6 and 5-HT7 receptor agents in the treatment of Alzheimer's disease
    Authors:
    Katarzyna Kucwaj-Brysz, Hanna Baltrukevich, Kinga Czarnota, Jadwiga Handzlik
    Academic press:
    Bioorganic & Medicinal Chemistry Letters (rok: 2021, tom: 49, strony: 45300), Wydawca: Elsevier
    Status:
    Published
    DOI:
    10.1016/j.bmcl.2021.128275 - link to the publication
  2. Chlorine substituents and linker topology as factors of 5-HT6R activity for novel highly active 1,3,5-triazine derivatives with procognitive properties in vivo
    Authors:
    Sylwia Sudoł, Katarzyna Kucwaj-Brysz, Rafał Kurczab, Natalia Wilczyńska, Magdalena Jastrzębska-Więsek, Grzegorz Satała, Gniewomir Latacz, Monika Głuch-Lutwin, Barbara Mordyl, Ewa Żesławska, Wojciech Nitek, Anna Partyka, Kamila Buzun, Agata Doroz-Płonka, Anna Wesołowska, Anna Bielawska, Jadwiga Handzlik
    Academic press:
    European Journal of Medicinal Chemistry (rok: 2020, tom: 203, strony: 45307), Wydawca: Elsevier
    Status:
    Published
    DOI:
    10.1016/j.ejmech.2020.112529 - link to the publication
  3. Discovery of phenylselenoether-hydantoin hybrids as ABCB1 efflux pump modulating agents with cytotoxic and antiproliferative actions in resistant T-lymphoma
    Authors:
    Wesam Ali, Gabriella Spengler, Annamaria Kincses, Marta Nove , Cecilia Battistelli, Gniewomir Latacz, Małgorzata Starek , Monika Dąbrowska, Ewelina Honkisz-Orzechowska, Annalisa Romanelli, Manuela Monica Rasile, Ewa Szymanska, Claus Jacob, Clemens Zwergel, Jadwiga Handzlik
    Academic press:
    European Journal of Medicinal Chemistry (rok: 2020, tom: 200, strony: 45308), Wydawca: Elsevier
    Status:
    Published
    DOI:
    10.1016/j.ejmech.2020.112435 - link to the publication
  4. First-in-Class Selenium-Containing Potent Serotonin Receptor 5-HT6 Agents with a Beneficial Neuroprotective Profile against Alzheimer's Disease
    Authors:
    Pyka P, Haberek W, Więcek M, Szymanska E, Ali W, Cios A, Jastrzębska-Więsek M, Satała G, Podlewska S, Di Giacomo S, Di Sotto A, Garbo S, Karcz T, Lambona C, Marocco F, Latacz G, Sudoł-Tałaj S, Mordyl B, Głuch-Lutwin M, Siwek A, Czarnota-Łydka K, Gogola D, Olejarz-Maciej A, Wilczyńska-Zawal N, Honkisz-Orzechowska E, Starek M, Dąbrowska M, Kucwaj-Brysz K, Fioravanti R, Nasim MJ, Hittinger M, Partyka A, Wesołowska A, Battistelli C, Zwergel C, Handzlik J.
    Academic press:
    Journal of Medicinal Chemistry (rok: 2024, tom: 67, strony: 1580-1610), Wydawca: ACS
    Status:
    Published
    DOI:
    10.1021/acs.jmedchem.3c02148 - link to the publication
  5. Multitargeting the action of 5-HT6 serotonin receptor ligands by additional modulation of kinases in the search for a new therapy for Alzheimer's Disease : can it work from a molecular point of vew?
    Authors:
    Czanota-Łydka Kinga, Kucwaj-Brysz Katarzyna, Pyka Patryk, Haberek Wawrzyniec, Podlewska Sabina, Handzlik Jadwiga.
    Academic press:
    International Journal of Molecular Sciences (rok: 2022, tom: 23, strony: 45315), Wydawca: MDPI
    Status:
    Published
    DOI:
    10.3390/ijms23158768 - link to the publication
  6. New Triazine Derivatives as Serotonin 5-HT6 Receptor Ligands
    Authors:
    Dorota Łażewska, , Małgorzata Więcek, Grzegorz Satała, Paulina Chałupnik , Ewa Żesławska, Ewelina Honkisz-Orzechowska, Monika Tarasek, Gniewomir Latacz , Wojciech Nitek, Ewa Szymańska, and Jadwiga Handzlik*
    Academic press:
    Molecules (rok: 2023, tom: 28, strony: 45312), Wydawca: MDPI
    Status:
    Published
    DOI:
    10.3390/molecules28031108 - link to the publication
  7. Synthesis, computational and experimental pharmacological studies for (thio)ether-triazine 5-HT6R ligands with noticeable action on AChE/BChE and chalcogen-dependent intrinsic activity in search for new class of drugs against Alzheimer's disease
    Authors:
    Kinga Czarnota-Łydka, Sylwia Sudoł-Tałaj, Katarzyna Kucwaj-Brysz, Rafał Kurczab, Grzegorz Satała, Modesto de Candia, Francesco Samarelli, Cosimo Damiano Altomare, Alessia Carocci, Alexia Barbarossa, Ewa Zesławska, Monika Głuch-Lutwin, Barbara Mordyl, Monika Kubacka, Natalia Wilczynska-Zawal, Magdalena Jastrzębska-Więsek, Anna Partyka, Nadia Khan, Małgorzata Więcek, Wojciech Nitek, Ewelina Honkisz-Orzechowska, Gniewomir Latacz , Anna Wesołowska, Antonio Carrieri, Jadwiga Handzlik*
    Academic press:
    European Journal of Medicinal Chemistry (rok: 2023, tom: 259, strony: 115695), Wydawca: Elsevier
    Status:
    Published
    DOI:
    10.1016/j.ejmech.2023.115695 - link to the publication
  8. An exit beyond the pharmacophore model for 5-HT6R agents - a new strategy to gain dual 5-HT6/5-HT2A action for triazine derivatives with procognitive potential
    Authors:
    Katarzyna Kucwaj-Brysz, Wesam Ali, Rafał Kurczab, Sylwia Sudoł-Tałaj, Natalia Wilczyńska-Zawal, Magdalena Jastrzębska-Więsek, Grzegorz Satała, Barbara Mordyl, Ewa Żesławska, Agnieszka Olejarz-Maciej, Kinga Czarnota, Gniewomir Latacz, Anna Partyka, Anna Wesołowska, Wojciech Nitek, Jadwiga Handzlik
    Academic press:
    Bioorganic Chemistry (rok: 2022, tom: 121, strony: 45307), Wydawca: Elsevier
    Status:
    Published
    DOI:
    10.1016/j.bioorg.2022.105695 - link to the publication
  9. Antitubercular polyhalogenated phenothiazines and phenoselenazine with reduced binding to CNS receptors
    Authors:
    Maria Giulia Nizi, Jenny Desantis, Yoshio Nakatani, Serena Massari, Maria Angela Mazzarella, Gauri Shetye, Stefano Sabatini, Maria Letizia Barreca, Giuseppe Manfroni, Tommaso Felicetti, Rowena Rushton-Green, Kiel Hards, Gniewomir Latacz, Grzegorz Satała, Andrzej J. Bojarski, Violetta Cecchetti, Michal H. Kolar , Jadwiga Handzlik, Gregory M. Cook, Scott G. Franzblau, Oriana Tabarrini
    Academic press:
    European Journal of Medicinal Chemistry (rok: 2020, tom: 201, strony: 45304), Wydawca: Elsevier
    Status:
    Published
    DOI:
    10.1016/j.ejmech.2020.112420 - link to the publication
  10. Are the Hydantoin-1,3,5-triazine 5-HT6R Ligands a Hope to a Find New Procognitive and Anti-Obesity Drug? Considerations Based on Primary In Vivo Assays and ADME-Tox Profile In Vitro
    Authors:
    Annamaria Lubelska, Gniewomir Latacz, Magdalena Jastrzębska-Więsek, Magdalena Kotańska, Rafał Kurczab, Anna Partyka, Małgorzata Anna Marć, Daria Wilczyńska, Agata Doroz-Płonka, Dorota Łażewska, Anna Wesołowska, Katarzyna Kieć-Kononowicz and Jadwiga Handzlik*
    Academic press:
    Molecules (rok: 2019, tom: 24, strony: 45315), Wydawca: MDPI
    Status:
    Published
    DOI:
    10.3390/molecules24244472 - link to the publication
  11. Hydrophobicity modulation via the substituents at positions 2 and 4 of 1,3,5-triazine to enhance therapeutic ability against Alzheimer's disease for potent serotonin 5-HT6R agents
    Authors:
    Sylwia Sudoł-Tałaj, Katarzyna Kucwaj-Brysz, Sabina Podlewska, Rafał Kurczab, Grzegorz Satała, Barbara Mordyl, Monika Głuch-Lutwin, Natalia Wilczyńska-Zawal, Magdalena Jastrzębska-Więsek, Kinga Czarnota-Łydka, Kinga Kurowska, Monika Kubacka, Ewa Żesławska, Wojciech Nitek, Agnieszka Olejarz-Maciej, Agata Doroz-Płonka, Anna Partyka, Gniewomir Latacz, Anna Wesołowska, Jadwiga Handzlik*
    Academic press:
    European Journal of Medicinal Chemistry (rok: 2023, tom: 260, strony: 115756), Wydawca: Elsevier
    Status:
    Published
    DOI:
    10.1016/j.ejmech.2023.115756 - link to the publication
  12. Seleno-vs. thioether triazine derivatives in search for new anticancer agents overcoming multidrug resistance in lymphoma
    Authors:
    Ali Wesam, Garbo Sabrina, Kincses Annamária, Nové Márta, Spengler Gabriella, Di Bello Elisabetta, Honkisz-Orzechowska Ewelina, Karcz Tadeusz, Szymańska Ewa, Żesławska Ewa, Starek Małgorzata, Dąbrowska Monika, Nitek Wojciech, Kucwaj-Brysz Katarzyna, Pyka Patryk, Fioravanti Rossella, Jacob Claus, Battistelli Cecilia, Zwergel Clemens, Handzlik Jadwiga.
    Academic press:
    European Journal of Medicinal Chemistry (rok: 2022, tom: 243, strony: 45310), Wydawca: Elsevier
    Status:
    Published
    DOI:
    10.1016/j.ejmech.2022.114761 - link to the publication
  13. The Phenoxyalkyltriazine Antagonists for 5‐HT6 Receptor with Promising Procognitive and Pharmacokinetic Properties In Vivo in Search for a Novel Therapeutic Approach to Dementia Diseases
    Authors:
    Sylwia Sudoł, Agnieszka Cios, Magdalena Jastrzębska‐Więsek, Ewelina Honkisz‐Orzechowska, Barbara Mordyl, Natalia Wilczyńska‐Zawal, Grzegorz Satała, Katarzyna Kucwaj‐Brysz, Anna Partyka, Gniewomir Latacz, Agnieszka Olejarz‐Maciej, Anna Wesołowska and Jadwiga Handzlik *
    Academic press:
    International Journal of Molecular Sciences (rok: 2021, tom: 22, strony: 14246), Wydawca: MDPI
    Status:
    Published
    DOI:
    10.3390/ijms221910773 - link to the publication

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