Tranylcypromine and 6-trifluoroethyl thienopyrimidine hybrid as LSD1 inhibitor.
Bioorg Med Chem Lett
; 29(6): 844-847, 2019 03 15.
Article
em En
| MEDLINE
| ID: mdl-30713023
ABSTRACT
Tranylcypromine moiety extracted from LSD1 inhibitors and 6-trifluoroethyl thienopyrimidine moiety from menin-MLL1 PPI inhibitors were merged to give new chemotypes for medicinal chemistry study. Among 15 new compounds prepared in this work, some exhibited nanomolar LSD1 activity and good selectivity over MAO-A/B, low micromolar menin-MLL1 PPI inhibitory activity, as well as submicromolar MV4-11 antiprofilative activities. Intracellular LSD1 engagement of compounds with higher enzymatic and antiproliferative activities was confirmed by CD86 mRNA up-regulation experiments.
Palavras-chave
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Pirimidinas
/
Tranilcipromina
/
Histona Desmetilases
/
Inibidores da Monoaminoxidase
/
Antineoplásicos
Idioma:
En
Ano de publicação:
2019
Tipo de documento:
Article