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

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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