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Heteroaryl-linked 5-(1H-benzimidazol-1-yl)-2-thiophenecarboxamides: Potent inhibitors of polo-like kinase 1 (PLK1) with improved drug-like properties |
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| Authors: | Tara R Rheault Kelly H Donaldson Jennifer G Badiang-Alberti Ronda G Davis-Ward C Webb Andrews Ramesh Bambal Jeffrey R Jackson Mui Cheung |
| Institution: | 1. GlaxoSmithKline, Five Moore Drive, Research Triangle Park, NC 27709, United States;2. GlaxoSmithKline, 1250 South Collegeville Road, Collegeville, PA 19426, United States;3. GlaxoSmithKline, 709 Swedeland Road, King of Prussia, PA 19406, United States |
| 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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