title: Discovery of thiophene inhibitors of polo-like kinase.
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.
authors.affiliation: Oncology R & D, GlaxoSmithKline, Five Moore Drive, PO Box 13398, Research Triangle Park, NC 27709, USA. kyle.a.emmitte@Vanderbilt.edu
authors.forename: Kyle A
authors.initials: KA
authors.lastname: Emmitte
authors.forename: C Webb
authors.initials: CW
authors.lastname: Andrews
authors.forename: Jennifer G
authors.initials: JG
authors.lastname: Badiang
authors.forename: Ronda G
authors.initials: RG
authors.lastname: Davis-Ward
authors.forename: Hamilton D
authors.initials: HD
authors.lastname: Dickson
authors.forename: David H
authors.initials: DH
authors.lastname: Drewry
authors.forename: Holly K
authors.initials: HK
authors.lastname: Emerson
authors.forename: Andrea H
authors.initials: AH
authors.lastname: Epperly
authors.forename: Daniel F
authors.initials: DF
authors.lastname: Hassler
authors.forename: Victoria B
authors.initials: VB
authors.lastname: Knick
authors.forename: Kevin W
authors.initials: KW
authors.lastname: Kuntz
authors.forename: Timothy J
authors.initials: TJ
authors.lastname: Lansing
authors.forename: James A
authors.initials: JA
authors.lastname: Linn
authors.forename: Robert A
authors.initials: RA
authors.lastname: Mook
authors.forename: Kristen E
authors.initials: KE
authors.lastname: Nailor
authors.forename: James M
authors.initials: JM
authors.lastname: Salovich
authors.forename: Glenn M
authors.initials: GM
authors.lastname: Spehar
authors.forename: Mui
authors.initials: M
authors.lastname: Cheung
mesh_terms: D000818:Animals; D002453:Cell Cycle; D018797:Cell Cycle Proteins / Q000037:antagonists & inhibitors* / Q000737:chemistry; D045744:Cell Line, Tumor; D049109:Cell Proliferation; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D006801:Humans; D020128:Inhibitory Concentration 50; D051379:Mice; D008938:Mitosis; D008956:Models, Chemical; D008968:Molecular Conformation; D017346:Protein Serine-Threonine Kinases / Q000037:antagonists & inhibitors* / Q000737:chemistry; D011518:Proto-Oncogene Proteins / Q000037:antagonists & inhibitors* / Q000737:chemistry; D013876:Thiophenes / Q000037:antagonists & inhibitors* / Q000737:chemistry; D000097869:Polo-Like Kinase 1
chemical_list: D018797:Cell Cycle Proteins; D004791:Enzyme Inhibitors; D017346:Protein Serine-Threonine Kinases; D011518:Proto-Oncogene Proteins; D013876:Thiophenes; D000097869:Polo-Like Kinase 1