1.
Bioorg Med Chem Lett
; 18(2): 634-9, 2008 Jan 15.
Artículo
en Inglés
| MEDLINE
| ID: mdl-18055203
RESUMEN
2-Amino-5-(thioaryl)thiazoles are potent inhibitors of TrkA (e.g., 20h, TrkA IC(50)=0.6 nM) that show anti-proliferative effect in cellular assays. A proposed inhibitor binding mode to TrkA active site is consistent with key SAR observations.
Asunto(s)
Receptor trkA/antagonistas & inhibidores , Tiazoles/farmacología , Fosforilación , Receptor trkA/metabolismo , Relación Estructura-Actividad , Tiazoles/química
2.
J Med Chem
; 48(7): 2258-61, 2005 Apr 07.
Artículo
en Inglés
| MEDLINE
| ID: mdl-15801816
RESUMEN
A series of fluoroglycosylated fluoroindolocarbazoles was examined with respect to their topoisomerase I activity, cytotoxicity, and selectivity. The lead clinical candidate from this series, BMS-250749, displays broad spectrum antitumor activity superior to CPT-11 against some preclinical xenograft models, including curative antitumor activity against Lewis lung carcinoma.