Discovery of thiophene inhibitors of polo-like kinase

The discovery and development of a series of thiophenes as potent and selective inhibitors of PLK is described. Identification and characterization of 2, a useful in vitro PLK inhibitor tool compound, is also presented.

Gespeichert in:

Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2009-02, Vol.19 (3), p.1018-1021
Hauptverfasser:	Emmitte, Kyle A., Andrews, C. Webb, Badiang, Jennifer G., Davis-Ward, Ronda G., Dickson, Hamilton D., Drewry, David H., Emerson, Holly K., Epperly, Andrea H., Hassler, Daniel F., Knick, Victoria B., Kuntz, Kevin W., Lansing, Timothy J., Linn, James A., Mook, Robert A., Nailor, Kristen E., Salovich, James M., Spehar, Glenn M., Cheung, Mui
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antineoplastic agents Benzimidazole Biological and medical sciences Cell Cycle Cell Cycle Proteins - antagonists & inhibitors Cell Cycle Proteins - chemistry Cell Line, Tumor Cell Proliferation Chemistry, Pharmaceutical - methods Drug Design Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - pharmacology General aspects Humans Inhibitor Inhibitory Concentration 50 Medical sciences Mice Mitosis Models, Chemical Molecular Conformation Pharmacology. Drug treatments Polo-like kinase Polo-Like Kinase 1 Protein Serine-Threonine Kinases - antagonists & inhibitors Protein Serine-Threonine Kinases - chemistry Proto-Oncogene Proteins - antagonists & inhibitors Proto-Oncogene Proteins - chemistry Thiophene Thiophenes - antagonists & inhibitors Thiophenes - chemistry
Online-Zugang:	Volltext
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!

Beschreibung
Zusammenfassung:	The discovery and development of a series of thiophenes as potent and selective inhibitors of PLK is described. Identification and characterization of 2, a useful in vitro PLK inhibitor tool compound, is also presented.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2008.11.041