PUBLICATION
Multicomponent Synthesis and Binding Mode of Imidazo[1,2- a]pyridine-Capped Selective HDAC6 Inhibitors
- Authors
- Mackwitz, M.K.W., Hamacher, A., Osko, J.D., Held, J., Schöler, A., Christianson, D.W., Kassack, M.U., Hansen, F.K.
- ID
- ZDB-PUB-180526-4
- Date
- 2018
- Source
- Organic letters 20(11): 3255-3258 (Journal)
- Registered Authors
- Keywords
- none
- MeSH Terms
-
- Pyridines/chemistry*
- Imidazoles
- Histone Deacetylase Inhibitors
- Histone Deacetylase 6/antagonists & inhibitors*
- Zebrafish
- Zebrafish Proteins/antagonists & inhibitors*
- Molecular Structure
- Animals
- PubMed
- 29790770 Full text @ Org. Lett.
Citation
Mackwitz, M.K.W., Hamacher, A., Osko, J.D., Held, J., Schöler, A., Christianson, D.W., Kassack, M.U., Hansen, F.K. (2018) Multicomponent Synthesis and Binding Mode of Imidazo[1,2- a]pyridine-Capped Selective HDAC6 Inhibitors. Organic letters. 20(11):3255-3258.
Abstract
The multicomponent synthesis of a mini-library of histone deacetylase inhibitors with imidazo[1,2- a]pyridine-based cap groups is presented. The biological evaluation led to the discovery of the hit compound MAIP-032 as a selective HDAC6 inhibitor with promising anticancer activity. The X-ray structure of catalytic domain 2 from Danio rerio HDAC6 complexed with MAIP-032 revealed a monodentate zinc-binding mode.
Genes / Markers
Expression
Phenotype
Mutations / Transgenics
Human Disease / Model
Sequence Targeting Reagents
Fish
Orthology
Engineered Foreign Genes
Mapping