Design And Synthesis of 2-Amino-Pyrazolopyridines As Polo-Like Kinase 1 Inhibitors

Design And Synthesis of 2-Amino-Pyrazolopyridines As Polo-Like Kinase 1 Inhibitors

A series of 2-amino-pyrazolopyridines was designed and synthesized as Polo-like kinase (Plk) inhibitors based on a low micromolar hit. The SAR was developed to provide compounds exhibiting low nanomolar inhibitory activity of Plk1; the phenotype of treated cells is consistent with Plk1 inhibition. A...

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Veröffentlicht in:Bioorganic & medicinal chemistry 2009-05, Vol.18 (20)
Hauptverfasser: Fucini, R.V., Hanan, E.J., Romanowski, M.J., Elling, R.A., Lew, W., Barr, K.J., Zhu, J., Yoburn, J.C., Liu, Y., Fahr, B.T., Fan, J., Lu, Y., Pham, P., Choong, I.C., VanderPorten, E.C., Bui, M., Purkey, H.E., Evanchik, M.J., Yang, W.
Format: Artikel
Sprache:eng
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BASIC BIOLOGICAL SCIENCES
DESIGN
Other,OTHER, BIO, CHEM
PHENOTYPE
PHOSPHOTRANSFERASES
SYNTHESIS
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Zusammenfassung:A series of 2-amino-pyrazolopyridines was designed and synthesized as Polo-like kinase (Plk) inhibitors based on a low micromolar hit. The SAR was developed to provide compounds exhibiting low nanomolar inhibitory activity of Plk1; the phenotype of treated cells is consistent with Plk1 inhibition. A co-crystal structure of one of these compounds with zPlk1 confirms an ATP-competitive binding mode.
ISSN:0968-0896
1464-3391