Discovery of 5-pyrrolopyridinyl-2-thiophenecarboxamides as potent AKT kinase inhibitors
A pyrrolopyridinyl thiophene carboxamide 7 was discovered as a tractable starting point for a lead optimization effort in an AKT kinase inhibition program. SAR studies aided by a co-crystal structure of 7 in AKT2 led to the identification of AKT inhibitor
Seefeld, Mark A.,Rouse, Meagan B.,McNulty, Kenneth C.,Sun, Lihui,Wang, Jizhou,Yamashita, Dennis S.,Luengo, Juan I.,Zhang, ShuYun,Minthorn, Elisabeth A.,Concha, Nestor O.,Heerding, Dirk A.
scheme or table
p. 2244 - 2248
(2009/12/07)
INHIBITORS OF Akt ACTIVITY
Invented are novel thiophene compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.
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Page/Page column 92
(2010/11/27)
Novel thienopyrrole glycogen phosphorylase inhibitors: Synthesis, in vitro SAR and crystallographic studies
Two series of novel thienopyrrole inhibitors of recombinant human liver glycogen phosphorylase a (GPa) which are effective in reducing glucose output from rat hepatocytes are described. Representative compounds have been shown to bind at the dimer interface site of the rabbit muscle enzyme by X-ray crystallography.
Whittamore, Paul R.O.,Addie, Matthew S.,Bennett, Stuart N.L.,Birch, Alan M.,Butters, Michael,Godfrey, Linda,Kenny, Peter W.,Morley, Andrew D.,Murray, Paul M.,Oikonomakos, Nikos G.,Otterbein, Ludovic R.,Pannifer, Andrew D.,Parker, Jeremy S.,Readman, Kristy,Siedlecki, Pawel S.,Schofield, Paul,Stocker, Andy,Taylor, Melvyn J.,Townsend, Linda A.,Whalley, David P.,Whitehouse, Jennifer
p. 5567 - 5571
(2007/10/03)
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