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  • Title: Identification of novel, potent and selective inhibitors of Polo-like kinase 1.
    Author: Chen S, Bartkovitz D, Cai J, Chen Y, Chen Z, Chu XJ, Le K, Le NT, Luk KC, Mischke S, Naderi-Oboodi G, Boylan JF, Nevins T, Qing W, Chen Y, Wovkulich PM.
    Journal: Bioorg Med Chem Lett; 2012 Jan 15; 22(2):1247-50. PubMed ID: 22172702.
    Abstract:
    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.
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