1.
Bioorg Med Chem Lett
; 16(1): 96-9, 2006 Jan 01.
Artículo
en Inglés
| MEDLINE
| ID: mdl-16216502
RESUMEN
We report the synthesis of kinase targeted libraries based on the thienopyrazole scaffold. Several thienopyrazole analogs have been identified as submicromolar inhibitors of KDR.
Asunto(s)
Química Farmacéutica/métodos , Diseño de Fármacos , Inhibidores Enzimáticos/farmacología , Fosfotransferasas/química , Pirazoles/química , Pirazoles/síntesis química , Receptor 2 de Factores de Crecimiento Endotelial Vascular/antagonistas & inhibidores , Receptor 2 de Factores de Crecimiento Endotelial Vascular/química , Evaluación Preclínica de Medicamentos , Inhibidores Enzimáticos/química , Humanos , Concentración 50 Inhibidora , Modelos Químicos
2.
Comb Chem High Throughput Screen
; 5(8): 631-43, 2002 Dec.
Artículo
en Inglés
| MEDLINE
| ID: mdl-12470260
RESUMEN
NMR has proven to be a valuable tool for identifying small molecule drug leads that serve as starting points for lead optimization programs. In addition, NMR screening can also be applied during lead optimization in order to improve the pharmacokinetic properties of a compound. In this paper we review the NMR methods that can be used for this purpose. Several examples are then summarized to demonstrate the usefulness of fragment-based approaches in optimizing the physical properties of potential drug candidates.