Discovery of thiophene inhibitors of polo-like kinase

  • Bioorg Med Chem Lett. 2009 Feb 1;19(3):1018-21. doi: 10.1016/j.bmcl.2008.11.041.
Kyle A Emmitte  1 ,  C Webb Andrews ,  Jennifer G Badiang ,  Ronda G Davis-Ward ,  Hamilton D Dickson ,  David H Drewry ,  Holly K Emerson ,  Andrea H Epperly ,  Daniel F Hassler ,  Victoria B Knick ,  Kevin W Kuntz ,  Timothy J Lansing ,  James A Linn ,  Robert A Mook Jr ,  Kristen E Nailor ,  James M Salovich ,  Glenn M Spehar ,  Mui Cheung
Affiliations
  • 1. Oncology R & D, GlaxoSmithKline, Five Moore Drive, PO Box 13398, Research Triangle Park, NC 27709, USA. [email protected]
PMID: 19097784 DOI: 10.1016/j.bmcl.2008.11.041
Abstract

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.