Synthesis of Carboxamide-Containing Tranylcypromine Analogues as LSD1 (KDM1A) Inhibitors Targeting Acute Myeloid Leukemia.
FAD-dependent enzymes
acute myeloid leukemia
enzyme inhibitors
epigenetics
histone demethylases
Journal
ChemMedChem
ISSN: 1860-7187
Titre abrégé: ChemMedChem
Pays: Germany
ID NLM: 101259013
Informations de publication
Date de publication:
20 04 2021
20 04 2021
Historique:
revised:
18
12
2020
received:
22
09
2020
pubmed:
4
2
2021
medline:
12
1
2022
entrez:
3
2
2021
Statut:
ppublish
Résumé
Lysine-specific demethylase 1 (LSD1/KDM1A) oxidatively removes methyl groups from histone proteins, and its aberrant activity has been correlated with cancers including acute myeloid leukemia (AML). We report a novel series of tranylcypromine analogues with a carboxamide at the 4-position of the aryl ring. These compounds, such as 5 a and 5 b with benzyl and phenethylamide substituents, respectively, had potent sub-micromolar IC
Identifiants
pubmed: 33533576
doi: 10.1002/cmdc.202000754
doi:
Substances chimiques
Antineoplastic Agents
0
Enzyme Inhibitors
0
Tranylcypromine
3E3V44J4Z9
Histone Demethylases
EC 1.14.11.-
KDM1A protein, human
EC 1.5.-
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
1316-1324Informations de copyright
© 2021 Wiley-VCH GmbH.
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