1.
Bioorg Med Chem Lett
; 15(24): 5407-11, 2005 Dec 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-16216509
RESUMO
A novel series of potent inhibitors of Ras farnesyl transferase possessing a 1,2,4-triazole pharmacophore is described. These inhibitors were discovered from a parallel synthesis effort and were subsequently optimized to in vitro IC(50) value of less than 1nM.
Assuntos
Inibidores Enzimáticos/síntese química , Farnesiltranstransferase/antagonistas & inibidores , Triazóis/síntese química , Sequência de Aminoácidos , Inibidores Enzimáticos/farmacologia , Farnesiltranstransferase/genética , Genes ras , Modelos Moleculares , Conformação Molecular , Oligopeptídeos/química , Triazóis/farmacologia
2.
Bioorg Med Chem Lett
; 13(9): 1543-7, 2003 May 05.
Artigo
em Inglês
| MEDLINE
| ID: mdl-12699751
RESUMO
The evaluation of structure-activity relationships associated with the modification of the R115777 quinolinone ring moiety displaying potent in vitro inhibiting activity is described.