Discovery of 6-benzamide Containing 4-phenylquinazoline Derivatives as Novel PI3Kδ Inhibitors
Discovery of 6-benzamide Containing 4-phenylquinazoline Derivatives as Novel PI3Kδ Inhibitors
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含有 4-苯基喹唑啉衍生物的 6-苯甲酰胺作为新型 PI3K δ 抑制剂的发现
DOI：
10.2174/1570180813666160720160523
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发表时间：
2017-01-01
影响因子：
1
通讯作者：
Zhang, San-Qi
中科院分区：
文献类型：
--
作者：
Xin, Minhang;Hei, Yuan-Yuan;Zhang, San-Qi
本论文设计并合成了一系列新的6-苯甲酰胺基4-苯基喹唑啉衍生物作为PI 3 K δ抑制剂。建立了该系列化合物的初步SAR。PI 3 K δ抑制活性测定结果表明，大部分化合物对PI 3 K δ具有明显的抑制活性。化合物12 h是最有效的PI 3 K δ抑制剂，显示出17 nM的IC 50值。这些结果表明，6-苯甲酰胺含有4-苯基喹唑啉是一个令人鼓舞的化学亚结构，值得进一步的结构探索，以确定新的和高效的PI 3 K δ抑制剂。
In the present study, a series of new 6-benzamide containing 4-phenylquinazoline derivatives were designed and synthesized as PI3K delta inhibitors. The preliminary SAR for this series of compounds was established. PI3K delta inhibitory assay showed that most of the synthesized compounds achieved significant activity against PI3K delta. Compound 12h was the most potent PI3K delta inhibitor, displaying an IC50 value of 17 nM. These results reveal that the 6-benzamide containing 4-phenylquinazoline is an encouraging chemical substructure, deserving further structural exploration to identify novel and highly potent PI3K delta inhibitors.