噻吩并[2,3-d]嘧啶类化合物作为 B-Raf 抑制剂的发现和优化。
Discovery and optimization of thieno[2,3-d]pyrimidines as B-Raf inhibitors.
机构信息
Celgene Corporation, San Diego, 4550 Towne Centre Ct, San Diego, CA 92121, United States.
出版信息
Bioorg Med Chem Lett. 2012 Jan 1;22(1):747-52. doi: 10.1016/j.bmcl.2011.03.006. Epub 2011 Mar 6.
PMID:22137342
Abstract
The serine/threonine specific protein kinase B-Raf is part of the MAPK pathway and is an interesting oncology target. We have identified thieno[2,3-d]pyrimidines as a core scaffold of small molecule B-Raf inhibitors. The SAR of analogs in this series will be described.
摘要
丝氨酸/苏氨酸特异性蛋白激酶 B-Raf 是 MAPK 通路的一部分，是一个有趣的肿瘤靶点。我们已经确定噻吩并[2,3-d]嘧啶是小分子 B-Raf 抑制剂的核心骨架。本系列类似物的 SAR 将被描述。
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