Design, synthesis and biological evaluation of pyridazino[3,4,5-de]quinazolin-3(2H)-one as a new class of PARP-1 inhibitors.
Design, synthesis and biological evaluation of pyridazino[3,4,5-de]quinazolin-3(2H)-one as a new class of PARP-1 inhibitors.
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DOI：
10.1016/j.bmcl.2015.04.013
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发表时间：
2015-06
影响因子：
2.7
通讯作者：
Jie Wang;Hailiang Tan;Qi Sun;Z. Ge;Xin Wang;Yinye Wang;Runtao Li
中科院分区：
文献类型：
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作者：
Jie Wang;Hailiang Tan;Qi Sun;Z. Ge;Xin Wang;Yinye Wang;Runtao Li
设计并合成了一系列哒嗪并[3,4,5-去]喹唑啉-3(2H)-酮衍生物作为PARP-1抑制剂。大多数合成的化合物对 PARP-1 表现出良好的抑制活性，其中四种化合物的 IC50 值范围为 0.0914 μM 至 0.244 μM。进一步测试了两种化合物1a和1b在H2O2损伤的PC12细胞模型中的神经保护作用，两者均表现出优异的活性。
A series of pyridazino[3,4,5-de]quinazolin-3(2H)-one derivatives were designed and synthesized as PARP-1 inhibitors. Most of the synthesized compounds showed good inhibitory activities of PARP-1 and four of them achieved at the IC50values ranging from 0.0914 μM to 0.244 μM. Two compounds,1aand1b, were further tested for their neuroprotective effect in the PC12 cell model injured by H2O2and both of them exhibited excellent activities.