作为脾酪氨酸激酶（Syk）抑制剂的高效且选择性的吡唑基嘧啶
Highly potent and selective pyrazolylpyrimidines as Syk kinase inhibitors.
作者信息
Choi Jang-Sik, Hwang Hae-Jun, Kim Se-Won, Lee Byung Il, Lee Jaekyoo, Song Ho-Juhn, Koh Jong Sung, Kim Jung-Ho, Lee Phil Ho
机构信息
Department of Chemistry, Kangwon National University, Chuncheon 200-701, Republic of Korea; Oscotec Inc., 694-1 Sampyeong-dong, Bundang-gu, Seongnam-si, Gyeonggi-do 463-400, Republic of Korea.
Oscotec Inc., 694-1 Sampyeong-dong, Bundang-gu, Seongnam-si, Gyeonggi-do 463-400, Republic of Korea.
出版信息
Bioorg Med Chem Lett. 2015 Oct 15;25(20):4441-6. doi: 10.1016/j.bmcl.2015.09.011. Epub 2015 Sep 8.
A series of pyrazolylpyrimidine scaffold based Syk inhibitors were synthesized and evaluated for their biological activities and selectivity. Lead optimization efforts provided compounds with potent Syk inhibition in both enzymatic and TNF-α release assay.
合成了一系列基于吡唑基嘧啶骨架的Syk抑制剂，并对其生物活性和选择性进行了评估。先导化合物优化工作得到了在酶活性测定和TNF-α释放测定中均具有强效Syk抑制作用的化合物。
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