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. 2014 May 23;77(5):1117-22.
doi: 10.1021/np400856h. Epub 2014 May 5.

Acridone alkaloids from Glycosmis chlorosperma as DYRK1A inhibitors

Mehdi A Beniddir  1 , Erell Le Borgne, Bogdan I Iorga, Nadège Loaëc, Olivier Lozach, Laurent Meijer, Khalijah Awang, Marc Litaudon
Affiliations

Acridone alkaloids from Glycosmis chlorosperma as DYRK1A inhibitors

Mehdi A Beniddir et al. J Nat Prod. .

Abstract

Two new acridone alkaloids, chlorospermines A and B (1 and 2), were isolated from the stem bark of Glycosmis chlorosperma, together with the known atalaphyllidine (3) and acrifoline (4), by means of bioguided isolation using an in vitro enzyme assay against DYRK1A. Acrifoline (4) and to a lesser extent chlorospermine B (2) and atalaphyllidine (3) showed significant inhibiting activity on DYRK1A with IC50's of 0.075, 5.7, and 2.2 μM, respectively. Their selectivity profile was evaluated against a panel of various kinases, and molecular docking calculations provided structural details for the interaction between these compounds and DYRK1A.

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