Abstract:
:The identification of a novel series of PKCθ inhibitors and subsequent optimization using docking based on a crystal structure of PKCθ is described. SAR was rapidly generated around an amino pyridine-ketone hit; (6-aminopyridin-2-yl)(2-aminopyridin-3-yl)methanone 2 leading to compound 21 which significantly inhibits production of IL-2 in a mouse SEB-IL2 model.
journal_name
Bioorg Med Chem Lettjournal_title
Bioorganic & medicinal chemistry lettersauthors
Jimenez JM,Davis C,Boyall D,Fraysse D,Knegtel R,Settimo L,Young S,Bolton C,Chiu P,Curnock A,Rasmussen R,Tanner A,Ager Idoi
10.1016/j.bmcl.2012.05.114subject
Has Abstractpub_date
2012-07-15 00:00:00pages
4645-9issue
14eissn
0960-894Xissn
1464-3405pii
S0960-894X(12)00726-3journal_volume
22pub_type
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