Journal Article

PUBDB-2025-01454

http://join2-wiki.gsi.de/foswiki/pub/Main/Artwork/join2_logo100x88.png Synthesis and evaluation of tetrahydrobenzo[cd]indole derivatives as glycogen phosphorylase inhibitors

Arunrattiyakorn, P. (Corresponding author) ; Juiprasert, C. ; Koulas, S. M. ; Boonsri, P. ; Aree, T. ; Yagi-Utsumi, M. ; Kato, K. ; Leonidas, D. D.

2025
Birkhäuser Boston Cambridge, Mass. [u.a.]

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Please use a persistent id in citations: doi:10.1007/s00044-025-03384-7

Abstract: A series of tetrahydrobenzo[cd]indole derivatives was synthesized by condensation of a fungal metabolite hyphodermin A, a naphtho[1,2-c]furan-3,9-dione derivative, and various anilines in methanol. Using this approach, ten analogs (3a–3j) were synthesized and tested as inhibitors against glycogen phosphorylase (GP). While compounds 3e and 3i bearing hydrophobic bromo and trifluoromethyl groups showed moderated inhibition (Ki = 32.3–57.4 μΜ), compound 3g with hydroxy group had the most potent activity with a Ki value of 7.9 ± 0.7 μΜ against human liver GPa. An X-ray crystallography study of the rabbit muscle GPb-3g complexes revealed that this inhibitor binds at a subsite within the indole binding site of GP which has not been previously observed to bind ligands.

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Contributing Institute(s):

1. EMBL-User (EMBL-User)

Research Program(s):

1. 6G3 - PETRA III (DESY) (POF4-6G3) (POF4-6G3)
2. iNEXT-Discovery - Infrastructure for transnational access and discovery in structural biology (871037) (871037)

Experiment(s):

1. PETRA Beamline P13 (PETRA III)

Appears in the scientific report 2025

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