New potent STS inhibitors based on fluorinated 4-(1-phenyl-1H-[1,2,3]triazol-4-yl)-phenyl sulfamates - Publikacja - MOST Wiedzy

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New potent STS inhibitors based on fluorinated 4-(1-phenyl-1H-[1,2,3]triazol-4-yl)-phenyl sulfamates

Abstrakt

A series of fluorinated analogs based on the frameworks of 4-(1- phenyl-1H-[1,2,3]triazol-4-yl)-phenyl sulfamates have been synthesized as steroid sulfatase (STS) inhibitors. The design of chemical structures of new potential STS inhibitors was supported by molecular docking techniques to identify potential interactions between inhibitors and amino acid residues located in the STS active site. The STS inhibitory potency was evaluated on STS isolated from human placenta. We found that compounds substituted with fluorine atom at the meta position demonstrated the highest inhibitory effects in enzymatic STS assay. The most active analog 12e – inhibited STS enzyme with the IC50 value of 36 nM.

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Wersja publikacji
Accepted albo Published Version
Licencja
Copyright (2019 Informa UK Limited, trading as Taylor & Francis Group)

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Kategoria:
Publikacja w czasopiśmie
Typ:
artykuły w czasopismach
Opublikowano w:
JOURNAL OF ASIAN NATURAL PRODUCTS RESEARCH nr 22, strony 1037 - 1044,
ISSN: 1028-6020
Język:
angielski
Rok wydania:
2019
Opis bibliograficzny:
Daśko M., Demkowicz S., Rachoń J., Biernacki K., Aszyk J., Kozak W., Masłyk M., Kubiński K.: New potent STS inhibitors based on fluorinated 4-(1-phenyl-1H-[1,2,3]triazol-4-yl)-phenyl sulfamates// JOURNAL OF ASIAN NATURAL PRODUCTS RESEARCH -Vol. 22,iss. 11 (2019), s.1037-1044
DOI:
Cyfrowy identyfikator dokumentu elektronicznego (otwiera się w nowej karcie) 10.1080/10286020.2019.1680642
Źródła finansowania:
Weryfikacja:
Politechnika Gdańska

wyświetlono 147 razy

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