Journal of Medicinal Chemistry p. 1251 - 1254 (2009)
Update date:2022-07-29
Topics:
Schroeder, Gretchen M.
An, Yongmi
Cai, Zhen-Wei
Chen, Xiao-Tao
Clark, Cheryl
Cornelius, Lyndon A. M.
Dai, Jun
Gullo-Brown, Johnni
Gupta, Ashok
Henley, Benjamin
Hunt, John T.
Jeyaseelan, Robert
Kamath, Amrita
Kim, Kyoung
Lippy, Jonathan
Lombardo, Louis J.
Manne, Veeraswamy
Oppenheimer, Simone
Sack, John S.
Schmidt, Robert J.
Shen, Guoxiang
Stefanski, Kevin
Tokarski, John S.
Trainor, George L.
Wautlet, Barri S.
Wei, Donna
Williams, David K.
Zhang, Yingru
Zhang, Yueping
Fargnoli, Joseph
Borzilleri, Robert M.
Substituted N-(4-(2-aminopyridin-4-yloxy)-3-fluoro-phenyl)- 1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamides were identified as potent and selective Met kinase inhibitors. Substitution of the pyridine 3-position gave improved enzyme potency, while substitution of the pyridone 4-position led to improved aqueous solubility and kinase selectivity. Analogue 10 demonstrated complete tumor stasis in a Met- dependent GTL-16 human gastric carcinoma xenograft model following oral administration. Because of its excellent in vivo efficacy and favorable pharmacokinetic and preclinical safety profiles, 10 has been advanced into phase I clinical trials.
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