4-Phenyl-7-azaindoles as potent and selective IKK2 inhibitors.
The synthesis and SAR of a novel series of IKK2 inhibitors are described. Modification around the hinge binding region of the 7-azaindole led to a series of potent and selective inhibitors with good cellular activity.
GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire, UK.
John
J
Liddle
Paul
P
Bamborough
Michael D
MD
Barker
Sebastien
S
Campos
Rick P C
RP
Cousins
Geoffrey J
GJ
Cutler
Heather
H
Hobbs
Duncan S
DS
Holmes
Chris
C
Ioannou
Geoff W
GW
Mellor
Mary A
MA
Morse
Jeremy J
JJ
Payne
John M
JM
Pritchard
Kathryn J
KJ
Smith
Daniel T
DT
Tape
Caroline
C
Whitworth
Richard A
RA
Williamson
D000255:Adenosine Triphosphate / Q000737:chemistry; D001665:Binding Sites; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015195:Drug Design; D006801:Humans; D051550:I-kappa B Kinase / Q000037:antagonists & inhibitors*; D007211:Indoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D008956:Models, Chemical; D008958:Models, Molecular; D015394:Molecular Structure; D011485:Protein Binding; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000737:chemistry
C023422:7-azaindole dimer; D007211:Indoles; D013449:Sulfonamides; D000255:Adenosine Triphosphate; D051550:I-kappa B Kinase