基于结构的吡唑并[1,5-a][1,3,5]三嗪衍生物的设计、合成及其作为蛋白激酶CK2强效抑制剂的研究
Structure-based design, synthesis, and study of pyrazolo[1,5-a][1,3,5]triazine derivatives as potent inhibitors of protein kinase CK2.
作者信息
Nie Zhe, Perretta Carin, Erickson Philip, Margosiak Stephen, Almassy Robert, Lu Jia, Averill April, Yager Kraig M, Chu Shaosong
机构信息
Department of Medicinal Chemistry, Polaris Pharmaceuticals Inc., San Diego, CA 92121, USA.
出版信息
Bioorg Med Chem Lett. 2007 Aug 1;17(15):4191-5. doi: 10.1016/j.bmcl.2007.05.041. Epub 2007 May 18.
The structure-based design, synthesis, and anticancer activity of novel inhibitors of protein kinase CK2 are described. Using pyrazolo[1,5-a][1,3,5]triazine as the core scaffold, a structure-guided series of modifications provided pM inhibitors with microM-level cytotoxic activity in cell-based assays with prostate and colon cancer cell lines.
描述了基于结构的蛋白激酶CK2新型抑制剂的设计、合成及抗癌活性。以吡唑并[1,5-a][1,3,5]三嗪为核心骨架，通过一系列基于结构的修饰，得到了在前列腺和结肠癌细胞系的细胞实验中具有微摩尔级细胞毒性活性的皮摩尔级抑制剂。
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