1.
Bioorg Med Chem Lett
; 18(18): 5130-3, 2008 Sep 15.
Artículo
en Inglés
| MEDLINE
| ID: mdl-18718756
RESUMEN
A novel series of 7-[1H-indol-2-yl]-2,3-dihydro-isoindol-1-ones designed to be inhibitors of VEGF-R2 kinase was synthesized and found to potently inhibit VEGF-R2 and Aurora-A kinases. The structure-based design, synthesis, and initial SAR of the series are discussed.
Asunto(s)
Indoles , Proteínas Serina-Treonina Quinasas/antagonistas & inhibidores , Proteínas Tirosina Quinasas Receptoras/antagonistas & inhibidores , Animales , Aurora Quinasa A , Aurora Quinasas , Técnicas Químicas Combinatorias , Diseño de Fármacos , Indoles/síntesis química , Indoles/farmacología , Ratones , Modelos Moleculares , Estructura Molecular , Relación Estructura-Actividad , Factores de Crecimiento Endotelial Vascular/metabolismo , Ensayos Antitumor por Modelo de Xenoinjerto
2.
Org Lett
; 9(19): 3821-4, 2007 Sep 13.
Artículo
en Inglés
| MEDLINE
| ID: mdl-17718497
RESUMEN
The N-amination of heterocyclic compounds 1a-k with O-benzoylhydroxylamine derivatives 5 was developed and demonstrated to be a superior alternative to existing N-amination methods. A structure-reactivity relationship study was performed on variously substituted O-benzoylhydroxylamine derivatives, leading to the discovery of the novel and more efficient aminating reagents 5h and 5i.