发现具有抗增殖活性的嘧啶并哒嗪衍生物作为有效的 PI3K 抑制剂。
Discovery of cinnoline derivatives as potent PI3K inhibitors with antiproliferative activity.
机构信息
Shanghai Key Laboratory of Molecular Catalysis and Innovative Materials, Department of Chemistry, Fudan University, Shanghai, China.
Shanghai Key Laboratory of Molecular Catalysis and Innovative Materials, Department of Chemistry, Fudan University, Shanghai, China.
出版信息
Bioorg Med Chem Lett. 2021 Sep 15;48:128271. doi: 10.1016/j.bmcl.2021.128271. Epub 2021 Jul 17.
Cinnoline is a potential pharmacophore which has rarely been reported for uses as PI3K inhibitors. In this study, a series of cinnoline derivatives were developed as PI3K inhibitors and evaluated for enzymatic and cellular activities. Most compounds displayed nanomolar inhibitory activities against PI3Ks, among which 25 displayed high LLE and micromolar inhibitory potency against three human tumor cell lines (IC = 0.264 μM, 2.04 μM, 1.14 μM).
噌啉是一种潜在的药效团，很少有报道将其用作 PI3K 抑制剂。在这项研究中，开发了一系列噌啉衍生物作为 PI3K 抑制剂，并对其酶和细胞活性进行了评估。大多数化合物对 PI3Ks 表现出纳摩尔抑制活性，其中 25 种对三种人肿瘤细胞系表现出高 LLE 和微摩尔抑制效力（IC=0.264μM，2.04μM，1.14μM）。
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