How to Separate Kinase Inhibition from Undesired Monoamine Oxidase A Inhibition—The Development of the DYRK1A Inhibitor AnnH75 from the Alkaloid Harmine

The β–carboline alkaloid harmine is a potent DYRK1A inhibitor, but suffers from undesired potent inhibition of MAO-A, which strongly limits its application. We synthesized more than 60 analogues of harmine, either by direct modification of the alkaloid or by de novo synthesis of β–carboline and rela...

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Bibliographic Details
Main Authors: Anne Wurzlbauer, Katharina Rüben, Ece Gürdal, Apirat Chaikuad, Stefan Knapp, Wolfgang Sippl, Walter Becker, Franz Bracher
Format: Article
Language:English
Published: MDPI AG 2020-12-01
Series:Molecules
Subjects:
Online Access:https://www.mdpi.com/1420-3049/25/24/5962