Worldwide Medicinal Chemistry, Pfizer Global Research and Development, 200 CambridgePark Drive, Cambridge, MA 02140, USA.
Bioorg Med Chem Lett. 2011 Aug 15;21(16):4758-61. doi: 10.1016/j.bmcl.2011.06.065. Epub 2011 Jun 22.
Synthesis, modeling and structure-activity relationship of indazoles as inhibitors of Tpl2 kinase are described. From a high throughput screening effort, we identified an indazole hit compound 5 that has a single digit micromolar Tpl2 activity. Through SAR modifications at the C3 and C5 positions of the indazole, we discovered compound 31 with good potency in LANCE assay and cell-based p-Erk assay.
本文描述了作为 Tpl2 激酶抑制剂的吲唑类化合物的合成、建模和构效关系。通过高通量筛选，我们发现吲唑类化合物 5 具有单位数微摩尔级的 Tpl2 活性。通过对吲唑的 C3 和 C5 位进行 SAR 修饰，我们发现化合物 31 在 LANCE 测定和基于细胞的 p-Erk 测定中具有良好的活性。
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