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.
Emmitte
Kyle A
KA
Oncology R & D, GlaxoSmithKline, Five Moore Drive, PO Box 13398, Research Triangle Park, NC 27709, USA. kyle.a.emmitte@Vanderbilt.edu
Andrews
C Webb
CW
Badiang
Jennifer G
JG
Davis-Ward
Ronda G
RG
Dickson
Hamilton D
HD
Drewry
David H
DH
Emerson
Holly K
HK
Epperly
Andrea H
AH
Hassler
Daniel F
DF
Knick
Victoria B
VB
Kuntz
Kevin W
KW
Lansing
Timothy J
TJ
Linn
James A
JA
Mook
Robert A
RA
Nailor
Kristen E
KE
Salovich
James M
JM
Spehar
Glenn M
GM
Cheung
Mui
M
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
D018797:Cell Cycle Proteins; D004791:Enzyme Inhibitors; D017346:Protein Serine-Threonine Kinases; D011518:Proto-Oncogene Proteins; D013876:Thiophenes; D000097869:Polo-Like Kinase 1