Millennium Pharmaceuticals Inc., 40 Landsdowne St., Cambridge MA 01239, United States.
Bioorg Med Chem Lett. 2010 Aug 15;20(16):4795-9. doi: 10.1016/j.bmcl.2010.06.110. Epub 2010 Jun 25.
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.
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。
