Design and synthesis of 2-amino-isoxazolopyridines as Polo-like kinase inhibitors.
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Hanan EJ, Fucini RV, Romanowski MJ, Elling RA, Lew W, Purkey HE, VanderPorten EC, Yang W
Design and synthesis of 2-amino-isoxazolopyridines as Polo-like kinase inhibitors.
Bioorg Med Chem Lett. 2008 Oct 1;18(19):5186-9. doi: 10.1016/j.bmcl.2008.08.091. Epub 2008 Aug 29.
- PubMed ID
- 18790636 [ View in PubMed]
- Abstract
A series of 2-amino-isoxazolopyridines was designed and synthesized as Polo-like kinase (Plk) inhibitors. Key SAR and crystallographic data are discussed. More advanced analogues inhibit Plk1 with good enzymatic activity and modest cell-based activity. Differential selectivity among the three Plk isoforms is observed.
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- Binding Properties
Drug Target Property Measurement pH Temperature (°C) 3-[3-chloro-5-(5-{[(1S)-1-phenylethyl]amino}isoxazolo[5,4-c]pyridin-3-yl)phenyl]propan-1-ol Serine/threonine-protein kinase PLK1 IC 50 (nM) 99 7.2 30 Details