Synthesis, Biological Evaluation and Docking Studies of 13-Epimeric 10-fluoro- and 10-Chloroestra-1,4-dien-3-ones as Potential Aromatase Inhibitors

Synthesis, Biological Evaluation and Docking Studies of 13-Epimeric 10-fluoro- and 10-Chloroestra-1,4-dien-3-ones as Potential Aromatase Inhibitors

Fluorination of 13-epimeric estrones and their 17-deoxy counterparts was performed with Selectfluor as the reagent. In acetonitrile or trifluoroacetic acid (TFA), 10β-fluoroestra-1,4-dien-3-ones were formed exclusively. Mechanistic investigations suggest that fluorinations occurred via SET...

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Bibliographic Details
Main Authors: Rebeka Jójárt, Péter Traj, Édua Kovács, Ágnes Horváth, Gyula Schneider, Mihály Szécsi, Attila Pál, Gábor Paragi, Erzsébet Mernyák
Format: Article
Language:English
Published: MDPI AG 2019-05-01
Series:Molecules
Subjects:
13α-estrone
Selectfluor
aromatase
docking
TEMPO
single electron transfer
Online Access:https://www.mdpi.com/1420-3049/24/9/1783

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