Synthesis of Carboxamide-Containing Tranylcypromine Analogues as LSD1 (KDM1A) Inhibitors Targeting Acute Myeloid Leukemia.
Autor: | Teresa Borrello M; School of Pharmacy, University of East Anglia, Norwich, NR4 7TJ, UK., Benelkebir H; School of Pharmacy, University of East Anglia, Norwich, NR4 7TJ, UK., Lee A; School of Pharmacy, University of East Anglia, Norwich, NR4 7TJ, UK., Hin Tam C; School of Pharmacy, University of East Anglia, Norwich, NR4 7TJ, UK., Shafat M; Norwich Medical School, University of East Anglia, Norwich, NR4 7TJ, UK., Rushworth SA; Norwich Medical School, University of East Anglia, Norwich, NR4 7TJ, UK., Bowles KM; Norwich Medical School, University of East Anglia, Norwich, NR4 7TJ, UK., Douglas L; Protein Core Facility and Cancer Sciences, Cancer Research UK Centre and Experimental Cancer Medicines Centre University of Southampton Southampton General Hospital, Southampton, SO16 6YD, UK., Duriez PJ; Protein Core Facility and Cancer Sciences, Cancer Research UK Centre and Experimental Cancer Medicines Centre University of Southampton Southampton General Hospital, Southampton, SO16 6YD, UK., Bailey S; Protein Core Facility and Cancer Sciences, Cancer Research UK Centre and Experimental Cancer Medicines Centre University of Southampton Southampton General Hospital, Southampton, SO16 6YD, UK., Crabb SJ; Protein Core Facility and Cancer Sciences, Cancer Research UK Centre and Experimental Cancer Medicines Centre University of Southampton Southampton General Hospital, Southampton, SO16 6YD, UK., Packham G; Protein Core Facility and Cancer Sciences, Cancer Research UK Centre and Experimental Cancer Medicines Centre University of Southampton Southampton General Hospital, Southampton, SO16 6YD, UK., Ganesan A; School of Pharmacy, University of East Anglia, Norwich, NR4 7TJ, UK. |
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Jazyk: | angličtina |
Zdroj: | ChemMedChem [ChemMedChem] 2021 Apr 20; Vol. 16 (8), pp. 1316-1324. Date of Electronic Publication: 2021 Feb 03. |
DOI: | 10.1002/cmdc.202000754 |
Abstrakt: | 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 (© 2021 Wiley-VCH GmbH.) |
Databáze: | MEDLINE |
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