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  • Title: Heteroaryl-linked 5-(1H-benzimidazol-1-yl)-2-thiophenecarboxamides: potent inhibitors of polo-like kinase 1 (PLK1) with improved drug-like properties.
    Author: Rheault TR, Donaldson KH, Badiang-Alberti JG, Davis-Ward RG, Andrews CW, Bambal R, Jackson JR, Cheung M.
    Journal: Bioorg Med Chem Lett; 2010 Aug 01; 20(15):4587-92. PubMed ID: 20594842.
    Abstract:
    Potent inhibitors of PLK1 with acceptable solubility, mouse iv clearance, and reduced CYP450 inhibition were identified. Drug-like properties were improved using a heteroaryl ring as a functional handle for manipulation of inhibitors' physiochemical and DMPK properties.
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