1.
Bioorg Med Chem Lett
; 13(15): 2587-90, 2003 Aug 04.
Artigo
em Inglês
| MEDLINE
| ID: mdl-12852972
RESUMO
A series of structurally novel benzothiazole based small molecule inhibitors of p56(lck) was prepared to elucidate their structure-activity relationships (SAR), selectivity and cell activity in the T-cell proliferation assay. BMS-350751 (2) and BMS-358233 (3) are identified as potent Lck inhibitors with excellent cellular activities against T-cell proliferation.
Assuntos
Anilidas/síntese química , Anilidas/farmacologia , Inibidores Enzimáticos/síntese química , Inibidores Enzimáticos/farmacologia , Proteína Tirosina Quinase p56(lck) Linfócito-Específica/antagonistas & inibidores , Tiazóis/síntese química , Tiazóis/farmacologia , Divisão Celular/efeitos dos fármacos , Cristalografia por Raios X , Humanos , Modelos Moleculares , Conformação Proteica , Relação Estrutura-Atividade , Linfócitos T/efeitos dos fármacos , Linfócitos T/enzimologia
2.
Bioorg Med Chem Lett
; 13(13): 2145-9, 2003 Jul 07.
Artigo
em Inglês
| MEDLINE
| ID: mdl-12798323
RESUMO
A series of structurally novel benzothiazole based small molecule inhibitors of p56(lck) were prepared to elucidate their structure-activity relationships (SARs), selectivity and cell activity in the T-cell proliferation assay. BMS-243117 (compound 2) is identified as a potent, and selective Lck inhibitor with good cellular activity (IC(50)=1.1 microM) against T-cell proliferation.