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