优化 5-乙烯基芳基-3-吡啶甲腈作为蛋白激酶 Cθ抑制剂。
Optimization of 5-vinylaryl-3-pyridinecarbonitriles as PKCtheta inhibitors.
机构信息
Wyeth Research, Pearl River, NY 10965, USA.
出版信息
Bioorg Med Chem Lett. 2010 Mar 15;20(6):1965-8. doi: 10.1016/j.bmcl.2010.01.119. Epub 2010 Jan 28.
PMID:20153643
Abstract
Analog 8, a 3-pyridinecarbonitrile with an (E)-2-[6-[(4-methylpiperazin-1-yl)methyl]pyridin-2-yl]vinyl group at C-5, had an IC(50) value of 1.1 nM for the inhibition of PKCtheta and potently blocked the production of IL-2 in both stimulated murine T cells (IC(50)=34 nM) and human whole blood (IC(50)=500 nM).
摘要
Analog 8，一种 3-吡啶甲腈，在 C-5 位具有一个（E）-2-[6-[(4-甲基哌嗪-1-基)甲基]吡啶-2-基]乙烯基基团，对 PKCtheta 的抑制作用的 IC50 值为 1.1 nM，并能有效阻断刺激的小鼠 T 细胞（IC50=34 nM）和人全血（IC50=500 nM）中 IL-2 的产生。
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