1.
Bioorg Med Chem Lett
; 19(1): 230-3, 2009 Jan 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-19027294
RESUMO
Anti-apoptotic Bcl-2 protects cells from apoptosis by binding to pro-apoptotic members of the Bcl-2 family thereby playing a role in tumour survival in response to chemo- or radiation therapy. We describe a series of phenyl pyrazoles that have high affinity for Bcl-2 and rationalise the observed SAR by means of an X-ray crystal structure.
Assuntos
Proteínas Proto-Oncogênicas c-bcl-2/antagonistas & inibidores , Pirazóis/síntese química , Tetra-Hidroisoquinolinas/química , Antineoplásicos/síntese química , Antineoplásicos/farmacologia , Apoptose/efeitos dos fármacos , Cristalografia por Raios X , Estrutura Molecular , Pirazóis/farmacologia , Relação Estrutura-Atividade , Tetra-Hidroisoquinolinas/farmacologia
2.
Bioorg Med Chem Lett
; 19(6): 1767-72, 2009 Mar 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-19217289
RESUMO
The separation of atropisomeric conformers of 1,2,3,4-tetrahydroisoquinoline amide Bcl-2 ligands allowed the identification of the bioactive conformer which was subsequently confirmed by X-ray crystallography.