发现并优化吡唑衍生物作为新型 Cdc25B 抑制剂。
Discovery and structural optimization of pyrazole derivatives as novel inhibitors of Cdc25B.
机构信息
The National Center for Drugs Screening, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
出版信息
Bioorg Med Chem Lett. 2010 May 1;20(9):2876-9. doi: 10.1016/j.bmcl.2010.03.040. Epub 2010 Mar 11.
Structural optimization and preliminary structure-activity relationship studies of a series of N-substituted maleimide fused-pyrazole analogues with Cdc25B inhibitory activity, starting from a high-throughput screening hit, are illustrated. A simplified 3,5-diacyl pyrazole analogue was obtained as the most potent compound (118, IC(50)=0.12 microM) with a 270-fold increase in potency.
从高通量筛选的命中化合物出发，对具有 Cdc25B 抑制活性的一系列 N-取代马来酰亚胺并吡唑类似物进行了结构优化和初步的结构-活性关系研究。得到了一种简化的 3,5-二酰基吡唑类似物，其活性最强（118，IC（50）=0.12 μM），活性提高了 270 倍。
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