1.
Bioorg Med Chem Lett
; 21(8): 2224-8, 2011 Apr 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-21441024
RESUMO
A new series of IGF-1R inhibitors related to hydantoins were identified from a lead originating from HTS. Their noncompetitive property as well as their slow binding characteristics provided a series of compounds with unique selectivity and excellent cellular activities.
Assuntos
Inibidores de Proteínas Quinases/química , Receptor IGF Tipo 1/antagonistas & inibidores , Trifosfato de Adenosina/química , Animais , Sítios de Ligação , Ligação Competitiva , Simulação por Computador , Avaliação Pré-Clínica de Medicamentos , Camundongos , Inibidores de Proteínas Quinases/síntese química , Inibidores de Proteínas Quinases/farmacocinética , Receptor IGF Tipo 1/metabolismo
2.
Chem Biol Drug Des
; 76(2): 100-6, 2010 Aug.
Artigo
em Inglês
| MEDLINE
| ID: mdl-20545947
RESUMO
From an azaindole lead, identified in high throughput screen, a series of potent bis-azaindole inhibitors of IGF1-R have been synthesized using rational drug design and SAR based on a in silico binding mode hypothesis. Although the resulting compounds produced the expected improved potency, the model was not validated by the co-crystallization experiments with IGF1-R.