Discovery of thieno[2,3-c]pyridines as potent COT inhibitors.
Evaluation of hit chemotypes from high throughput screening identified a novel series of 2,4-disubstituted thieno[2,3-c]pyridines as COT kinase inhibitors. Structural modifications exploring SAR at the 2- and 4-positions resulting in inhibitors with improved enzyme potency and cellular activity are disclosed.
George
Dawn
D
Abbott Bioresearch Center, 381 Plantation Street, Worcester, MA 01605, USA. dawn.george@abbott.com
Friedman
Michael
M
Allen
Hamish
H
Argiriadi
Maria
M
Barberis
Claude
C
Bischoff
Agnieszka
A
Clabbers
Anca
A
Cusack
Kevin
K
Dixon
Richard
R
Fix-Stenzel
Shannon
S
Gordon
Thomas
T
Janssen
Bernd
B
Jia
Yong
Y
Moskey
Maria
M
Quinn
Christopher
C
Salmeron
Jose-Andres
JA
Wishart
Neil
N
Woller
Kevin
K
Yu
Zhengtian
Z