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Bioorg Med Chem Lett
; 22(2): 1247-50, 2012 Jan 15.
Artículo
en Inglés
| MEDLINE
| ID: mdl-22172702
RESUMEN
A series of pyrimidodiazepines was identified as potent Polo-like kinase 1 (PLK1) inhibitors. The synthesis and SAR are discussed. The lead compound 7 (RO3280) has potent inhibitory activity against PLK1, good selectivity against other kinases, and excellent in vitro cellular potency. It showed strong antitumor activity in xenograft mouse models.