Wyeth Research, Chemical and Screening Sciences, 401 N. Middletown Road, Pearl River, NY 10965, USA.
Bioorg Med Chem Lett. 2009 Feb 1;19(3):766-9. doi: 10.1016/j.bmcl.2008.12.021. Epub 2008 Dec 10.
Thieno[2,3-b]pyridine-5-carbonitrile 16 with a 4-methyl-5-indolylamine at C-4 and a 5-methoxy-2-(dimethylamino)-methylphenyl group at C-2 had an IC(50) value of 16 nM for the inhibition of PKCtheta. While moderate inhibition of PKCdelta was also observed (IC(50)=130 nM), 16 had IC(50) values of greater than 5 microM against Lyn and other members of the Src kinase family.
噻吩并[2,3-b]吡啶-5-甲腈 16，在 C-4 位带有 4-甲基-5-吲哚基胺，在 C-2 位带有 5-甲氧基-2-（二甲基氨基）-甲氧基苯基，对 PKCtheta 的抑制作用的 IC50 值为 16 nM。虽然对 PKCdelta 的抑制作用也很明显（IC50=130 nM），但 16 对 Lyn 和 Src 激酶家族的其他成员的 IC50 值大于 5 microM。
