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

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

Abstract

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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Category:
Articles
Type:
artykuły w czasopismach
Published in:
JOURNAL OF ASIAN NATURAL PRODUCTS RESEARCH no. 22, pages 1037 - 1044,
ISSN: 1028-6020
Language:
English
Publication year:
2019
Bibliographic description:
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:
Digital Object Identifier (open in new tab) 10.1080/10286020.2019.1680642
Sources of funding:
Verified by:
Gdańsk University of Technology

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