1.
Bioorg Med Chem Lett
; 11(21): 2837-41, 2001 Nov 05.
Artigo
em Inglês
| MEDLINE
| ID: mdl-11597411
RESUMO
The first reported synthesis of the DNA-PK inhibitor 3-cyano-6-hydrazonomethyl-5-(4-pyridyl)pyrid-[1H]-2-one (OK-1035) is described. The structure of OK-1035 was validated by X-ray crystallography. An IC(50) value of 100 microM was determined for inhibition of DNA-PK, and this is approximately 12-fold higher than that reported previously.
Assuntos
Proteínas de Ligação a DNA , Inibidores Enzimáticos/farmacologia , Hidrazonas/farmacologia , Proteínas Serina-Treonina Quinases/antagonistas & inibidores , Piridonas/farmacologia , Cromonas/farmacologia , Cristalografia por Raios X , Proteína Quinase Ativada por DNA , Inibidores Enzimáticos/química , Hidrazonas/química , Modelos Moleculares , Morfolinas/farmacologia , Piridonas/química
2.
Bioorg Med Chem Lett
; 10(16): 1803-6, 2000 Aug 21.
Artigo
em Inglês
| MEDLINE
| ID: mdl-10969972
RESUMO
A weak HTS hit at the CCR2B receptor has been converted into a potent antagonist by array SAR studies. Selectivity over the closely related CCR5 receptor is also achieved.
