Synthesis, Docking Study and Kinase Inhibitory Activity of a Number of New Substituted Pyrazolo[3,4-c]pyridines.
Chem Pharm Bull (Tokyo)
; 65(1): 66-81, 2017.
Article
en En
| MEDLINE
| ID: mdl-28049917
ABSTRACT
A series of new pyrazolo[3,4-c]pyridines bearing various 1, 3, 5 or 1, 3, 7 pattern substitutions, were designed and synthesized. Some of them showed interesting inhibitory activity mainly against glycogen synthase kinase 3 (GSK3)α/ß as well as against cdc2-like kinases 1 (CLK1) and dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A), with good selectivity and remarkable structure-activity relationships (SARs), without being cytotoxic. Molecular simulations in correlation with biological data revealed the importance of the existence of N1-H as well as the absence of a bulky 7-substituent.
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Pirazoles
/
Piridinas
/
Proteínas Tirosina Quinasas
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Proteínas Serina-Treonina Quinasas
/
Inhibidores de Proteínas Quinasas
/
Simulación del Acoplamiento Molecular
Límite:
Humans
Idioma:
En
Revista:
Chem Pharm Bull (Tokyo)
Año:
2017
Tipo del documento:
Article