发现和优化 N-酰基和 N-芳酰基吡唑啉作为 B-Raf 激酶抑制剂。
Discovery and optimization of N-acyl and N-aroylpyrazolines as B-Raf kinase inhibitors.
机构信息
Millennium Pharmaceuticals Inc., 40 Landsdowne St., Cambridge MA 01239, United States.
出版信息
Bioorg Med Chem Lett. 2010 Aug 15;20(16):4795-9. doi: 10.1016/j.bmcl.2010.06.110. Epub 2010 Jun 25.
PMID:20630752
Abstract
A high throughput screen identified N-aroylpyrazoline 1 as a selective inhibitor of the V600E mutant of B-Raf kinase. Parallel synthesis of acyl, aroyl, and sulfonyl derivatives led to the identification of several potent inhibitors in both enzymatic and cellular (pERK) assays such as compound 42.
摘要
高通量筛选发现 N-芳酰基吡唑啉 1 是 V600E 突变型 B-Raf 激酶的选择性抑制剂。酰基、芳基和磺酰基衍生物的平行合成导致在酶和细胞（pERK）测定中鉴定出几种有效的抑制剂，如化合物 42。
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