Discovery of 4-morpholino-pyrimidin-6-one and 4-morpholino-pyrimidin-2-one-containing Phosphoinositide 3-kinase (PI3K) p110ß isoform inhibitors through structure-based fragment optimisation.
Bioorg Med Chem Lett
; 22(21): 6665-70, 2012 Nov 01.
Article
em En
| MEDLINE
| ID: mdl-23010274
ABSTRACT
The discovery of 4-morpholino-pyrimidin-6-one and 4-morpholino-pyrimidin-2-one-containing inhibitors of Phosphoinositide 3-kinases (PI3K) p110ß isoform is reported. Structure-based optimisation of the original fragment hit resulted in lead compounds with improvements in ligand efficiency, lipophilicity efficiency, p110ß potency and selectivity over p110α.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Inibidores Enzimáticos
/
Descoberta de Drogas
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Inibidores de Fosfoinositídeo-3 Quinase
Idioma:
En
Ano de publicação:
2012
Tipo de documento:
Article