Divergent synthesis of kinase inhibitor derivatives, leading to discovery of selective Gck inhibitors
Divergent synthesis of kinase inhibitor derivatives, leading to discovery of selective Gck inhibitors
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激酶抑制剂衍生物的不同合成，导致选择性 Gck 抑制剂的发现
DOI：
10.1016/j.bmcl.2017.03.055
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发表时间：
2017
期刊：
影响因子：
--
通讯作者：
Kan Toshiyuki
中科院分区：
文献类型：
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作者：
Matsumaru Takanori;Inai Makoto;Ishigami Kana;Iwamatsu Toshiki;Maita Hiroshi;Otsuguro Satoko;Nomura Takao;Matsuda Akira;Ichikawa Satoshi;Sakaitani Masahiro;Shuto Satoshi;Maenaka Katsumi;Kan Toshiyuki
我们通过钯催化的交叉偶联反应，将咪唑并[1,2-c]嘧啶和吲哚环化合物与芳香族（包括吡啶）衍生物缀合，完成了强效激酶抑制剂BAY 61-3606（1）和27种衍生物的发散合成。脾酪氨酸激酶（Syk）和生发中心激酶（Gck，MAP4K2）抑制测定表明，一些合成的化合物是选择性Gck抑制剂。
We accomplished divergent synthesis of potent kinase inhibitor BAY 61-3606 (1) and 27 derivatives via conjugation of imidazo[1,2-c]pyrimidine and indole ring compounds with aromatic (including pyridine) derivatives by means of palladium-catalyzed cross-coupling reaction. Spleen tyrosine kinase (Syk) and germinal center kinase (Gck, MAP4K2) inhibition assays showed that some of the synthesized compounds were selective Gck inhibitors.