Synthesis and structure–activity relationships of 2- and/or 4-halogenated 13β- and 13α-estrone derivatives as enzyme inhibitors of estrogen biosynthesis

Ring A halogenated 13α-, 13β-, and 17-deoxy-13α-estrone derivatives were synthesised with N-halosuccinimides as electrophile triggers. Substitutions occurred at positions C-2 and/or C-4. The potential inhibitory action of the halogenated estrones on human aromatase, steroid sulfatase, or 17β-hydroxy...

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Bibliographic Details
Main Authors: Ildikó Bacsa, Bianka Edina Herman, Rebeka Jójárt, Kevin Stefán Herman, János Wölfling, Gyula Schneider, Mónika Varga, Csaba Tömböly, Tea Lanišnik Rižner, Mihály Szécsi, Erzsébet Mernyák
Format: Article
Language:English
Published: Taylor & Francis Group 2018-01-01
Series:Journal of Enzyme Inhibition and Medicinal Chemistry
Subjects:
STS
Online Access:http://dx.doi.org/10.1080/14756366.2018.1490731