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Optimization of 5-phenyl-3-pyridinecarbonitriles as PKCθ inhibitors

Authors :
Boschelli, Diane H.
Wang, Daniel
Prashad, Amar S.
Subrath, Joan
Wu, Biqi
Niu, Chuan
Lee, Julie
Yang, Xiaoke
Brennan, Agnes
Chaudhary, Divya
Source :
Bioorganic & Medicinal Chemistry Letters. Jul2009, Vol. 19 Issue 13, p3623-3626. 4p.
Publication Year :
2009

Abstract

Abstract: The key intermediate, 4-chloro-5-iodo-3-pyridinecarbonitrile, allowed for ready optimization of the PKCθ inhibitory activity of a series of 3-pyridinecarbonitriles. Analog 13b with a 4-methylindol-5-ylamino group at C-4 and a 4-(2-(4-methylpiperazin-1-yl)ethoxy)phenyl group at C-5 had an IC50 value of 7.4nM for the inhibition of PKCθ. [Copyright &y& Elsevier]

Details

Language :
English
ISSN :
0960894X
Volume :
19
Issue :
13
Database :
Academic Search Index
Journal :
Bioorganic & Medicinal Chemistry Letters
Publication Type :
Academic Journal
Accession number :
41240881
Full Text :
https://doi.org/10.1016/j.bmcl.2009.04.126