Synthesis of 7,8-disubstituted benzolactam-V8 and its binding to protein kinase C.
Synthesis of 7,8-disubstituted benzolactam-V8 and its binding to protein kinase C.
复制标题
7,8-二取代苯并内酰胺-V8的合成及其与蛋白激酶C的结合。
DOI：
10.1016/s0960-894x(00)00609-0
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发表时间：
2001
影响因子：
2.7
通讯作者：
Blumberg,PM
中科院分区：
文献类型：
--
作者：
Ma,D;Zhang,T;Wang,G;Kozikowski,AP;Lewin,NE;Blumberg,PM
7-Methoxy-8-decynyl-benzolactam-V8 4 is synthesized using a catalytic asymmetric alkylation reaction as a key step. This compound shows potent activity to three PKC isozymes tested (Ki=45.6, 91.1, and 121.3nM to PKCα, δ, and ε, respectively), indicating that introduction of a suitable substituent at the 7-position of 8-decynyl-benzolactam-V8 only slightly reduces the PKC binding affinity.
