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Pure Diastereomers of a Tranylcypromine-Based LSD1 Inhibitor: Enzyme Selectivity and In-Cell Studies.
- Source :
-
ACS medicinal chemistry letters [ACS Med Chem Lett] 2014 Dec 08; Vol. 6 (2), pp. 173-7. Date of Electronic Publication: 2014 Dec 08 (Print Publication: 2015). - Publication Year :
- 2014
-
Abstract
- The pure four diastereomers (11a-d) of trans-benzyl (1-((4-(2-aminocyclopropyl)phenyl)amino)-1-oxo-3-phenylpropan-2-yl)carbamate hydrochloride 11, previously described by us as LSD1 inhibitor, were obtained by enantiospecific synthesis/chiral HPLC separation method. Tested in LSD1 and MAO assays, 11b (S,1S,2R) and 11d (R,1S,2R) were the most potent isomers against LSD1 and were less active against MAO-A and practically inactive against MAO-B. In cells, all the four diastereomers induced Gfi-1b and ITGAM gene expression in NB4 cells, accordingly with their LSD1 inhibition, and 11b and 11d inhibited the colony forming potential in murine promyelocytic blasts.
Details
- Language :
- English
- ISSN :
- 1948-5875
- Volume :
- 6
- Issue :
- 2
- Database :
- MEDLINE
- Journal :
- ACS medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 25699146
- Full Text :
- https://doi.org/10.1021/ml500424z