Borrello, T;
Tam, CH;
Shafat, M;
Rushworth, S;
Bowles, K;
Bailey, S;
Crabb, S;
... Douglas, L; + view all
(2020)
Synthesis of Carboxamides Tranylcypromine Analogues as LSD1 (KDM1A) Inhibitors for AML.
ChemRxiv: Cambridge, UK.
Preview |
Text
Shafat_synthesis-of-carboxamides-tranylcypromine-analogues-as-lsd1-kdm1a-inhibitors-for-aml.pdf Download (909kB) | Preview |
Abstract
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 containing a carboxamide at the 4-position of the aryl ring and novel carbamates. These compounds were potent submicromolar LSD1 inhibitors in enzyme assays and were anti-proliferative against a panel of AML cell lines. LSD1 target engagement in cells was demonstrated through the effects on H3K4me2 protein expression, CD86, CD11b and CD14 levels.
Archive Staff Only
 |
View Item |
