Inhibitory sulfatazy steroidowej na bazie amidosiarczanowych pochodnych 4-(1-fenylo-1H-[1,2,3]triazol-4-ylo)-fenolu jako potencjalne środki przeciwnowotworowe
Informacje szczegółowe
- Program finansujący:
- TANGO
- Instytucja:
- Narodowe Centrum Badań i Rozwoju (NCBR) (The National Centre for Research and Development)
- Porozumienie:
- TANGO-IV-A/0004/2019-00 z dnia 2020-08-28
- Okres realizacji:
- 2020-10-01 - 2022-12-31
- Kierownik projektu:
- dr inż. Mateusz Daśko
- Członkowie zespołu:
-
- Wykonawca dr hab. inż. Sebastian Demkowicz
- Kierownik dr inż. Mateusz Daśko
- Realizowany w:
- Katedra Chemii Nieorganicznej
- Wartość projektu:
- 250 000.00 PLN
- Typ zgłoszenia:
- Krajowy Program Badawczy
- Pochodzenie:
- Projekt krajowy
- Weryfikacja:
- Politechnika Gdańska
Publikacje powiązane z tym projektem
Filtry
wszystkich: 3
Katalog Projektów
Rok 2022
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Development of Sulfamoylated 4‑(1-Phenyl‑1H‑1,2,3-triazol-4-yl)phenol Derivatives as Potent Steroid Sulfatase Inhibitors for Efficient Treatment of Breast Cancer
PublikacjaWe present here the advances achieved in the development of new sulfamoylated 4-(1-phenyl-1H-1,2,3-triazol-4-yl)phenol derivatives as potent steroid sulfatase (STS) inhibitors for the treatment of breast cancer. Prompted by promising biological results and in silico analysis, the initial series of similar compounds were extended, appending a variety of m-substituents at the outer phenyl ring. The inhibition profiles of the newly...
Rok 2021
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New potent steroid sulphatase inhibitors based on 6-(1-phenyl-1H-1,2,3-triazol-4-yl)naphthalen-2-yl sulphamate derivatives
PublikacjaIn the present work, we report a new class of potent steroid sulphatase (STS) inhibitors based on 6-(1-phenyl-1H-1,2,3-triazol-4-yl)naphthalen-2-yl sulphamate derivatives. Within the set of new STS inhibitors, 6-(1-(1,2,3-trifluorophenyl)-1H-1,2,3-triazol-4-yl)naphthalen-2-yl sulphamate 3L demonstrated the highest activity in the enzymatic assay inhibiting the STS activity to 7.98% at 0.5 µM concentration. Furthermore, to verify...
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Novel 1,2,3-Triazole Derivatives as Mimics of Steroidal System—Synthesis, Crystal Structures Determination, Hirshfeld Surfaces Analysis and Molecular Docking
PublikacjaHerein, we present the synthesis and crystal structures determination of five 4-(1-phenyl-1H-1,2,3-triazol-4-yl)phenol derivatives containing halogen atoms, 6a–e, which may be used as an excellent mimic of steroids in the drug development process. Good quality crystals obtained for all of the synthesized compounds allowed the analysis of their molecular structures. Subsequently, the determined crystal structures were used to calculate...
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