1.
ACS Med Chem Lett
; 3(10): 850-5, 2012 Oct 11.
Artículo
en Inglés
| MEDLINE
| ID: mdl-24900389
RESUMEN
Optimization of a series of R132H IDH1 inhibitors from a high throughput screen led to the first potent molecules that show robust tumor 2-HG inhibition in a xenograft model. Compound 35 shows good potency in the U87 R132H cell based assay and â¼90% tumor 2-HG inhibition in the corresponding mouse xenograft model following BID dosing. The magnitude and duration of tumor 2-HG inhibition correlates with free plasma concentration.