Heteroaryl-linked 5-(1H-benzimidazol-1-yl)-2-thiophenecarboxamides: Potent inhibitors of polo-like kinase 1 (PLK1) with improved drug-like properties

GlaxoSmithKline, Research Triangle Park, NC 27709, USA.
Bioorganic & medicinal chemistry letters (Impact Factor: 2.33). 08/2010; 20(15):4587-92. DOI: 10.1016/j.bmcl.2010.06.009
Source: PubMed

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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