Design, synthesis and biological evaluation of substituted aminopyridazin-3(2 H )-ones as G0/G1-phase arresting agents with apoptosis-inducing activities
作者:Bing-Chen Ge、Hong-Fang Feng、Yu-Fang Cheng、Hai-Tao Wang、Bao-Ming Xi、Xue-Mei Yang、Jiang-Ping Xu、Zhong-Zhen Zhou
DOI:10.1016/j.ejmech.2017.09.077
日期:2017.12
series of aminopyridazin-3(2H)-one derivatives has been designed and synthesized. Their antiproliferative activities were evaluated against three human cancer cell lines (SH-SY5Y human neuroblastoma, K562 human myelogenous leukemia and AGS gastric cancer cell lines) using the MTT assay. The preliminary activity test displayed that compound 8a exhibited comparable activities against all test cells with
设计并合成了一系列氨基哒嗪-3(2H)-one衍生物。使用MTT法评估了它们对三种人类癌细胞系(SH-SY5Y人类神经母细胞瘤,K562人类骨髓性白血病和AGS胃癌细胞系)的抗增殖活性。初步活性测试表明,化合物8a对具有阳性对照氟尿嘧啶的所有测试细胞均表现出可比的活性。同时,化合物8b,8e和9c-e显示出对SH-SY5Y细胞的选择性抗增殖活性。此外,化合物8a-b的GI 50低 SH-SY5Y细胞诱导的凋亡值与SH-SY5Y细胞中的G0 / G1期细胞周期停滞有关,且呈剂量依赖性。