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氮杂芪类化合物作为强效且选择性的c-RAF抑制剂。

Aza-stilbenes as potent and selective c-RAF inhibitors.

作者信息

McDonald Octerloney, Lackey Karen, Davis-Ward Ronda, Wood Edgar, Samano Vicente, Maloney Patrick, Deanda Felix, Hunter Robert

机构信息

GlaxoSmithKline, Research Triangle Park, NC 27709, USA.

出版信息

Bioorg Med Chem Lett. 2006 Oct 15;16(20):5378-83. doi: 10.1016/j.bmcl.2006.07.063. Epub 2006 Aug 4.

DOI:10.1016/j.bmcl.2006.07.063
PMID:16890436
Abstract

The synthesis of several novel aza-stilbene derivatives was carried out. The compounds were tested for their c-RAF enzyme inhibition. Compound 27 possesses significant potency against c-RAF and demonstrates selectivity over other protein kinases. A hypothesis for the binding mode, activity, and selectivity is proposed.

摘要

合成了几种新型氮杂二苯乙烯衍生物。对这些化合物进行了c-RAF酶抑制测试。化合物27对c-RAF具有显著的活性，并对其他蛋白激酶表现出选择性。提出了关于其结合模式、活性和选择性的假说。

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