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B-RAF激酶的双结合位点抑制剂

Dual binding site inhibitors of B-RAF kinase.

作者信息

Wolin Ronald L, Bembenek Scott D, Wei Jianmei, Crawford Shelby, Lundeen Katherine, Brunmark Anders, Karlsson Lars, Edwards James P, Blevitt Jonathan M

机构信息

Johnson & Johnson Pharmaceutical Research & Development, L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA.

出版信息

Bioorg Med Chem Lett. 2008 May 1;18(9):2825-9. doi: 10.1016/j.bmcl.2008.04.002. Epub 2008 Apr 4.

DOI:10.1016/j.bmcl.2008.04.002
PMID:18434146
Abstract

Computer aided modeling guided the design of a series of diarylimidazole compounds (11-22) intended to interact with both the ATP and adjacent allosteric binding domains of B-RAF kinase. Their ability to inhibit the function of B-RAF kinase and intracellular ERK1/2 phosphorylation were evaluated.

摘要

计算机辅助建模指导了一系列二芳基咪唑化合物（11 - 22）的设计，这些化合物旨在与B - RAF激酶的ATP和相邻的变构结合域相互作用。评估了它们抑制B - RAF激酶功能和细胞内ERK1/2磷酸化的能力。

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