Identification of novel, potent and selective inhibitors of Polo-like kinase 1
S Chen, D Bartkovitz, J Cai, Y Chen, Z Chen… - Bioorganic & medicinal …, 2012 - Elsevier
S Chen, D Bartkovitz, J Cai, Y Chen, Z Chen, XJ Chu, K Le, NT Le, KC Luk, S Mischke…
Bioorganic & medicinal chemistry letters, 2012•ElsevierA 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.
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.
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.
Elsevier