Chem Biol Drug Des. 2012 Mar;79(3):360-7. doi: 10.1111/j.1747-0285.2011.01307.x.
A series of novel 2-(4-(2,4-dimethoxybenzoyl)phenoxy)-1-(4-(3-(piperidin-4-yl)propyl) piperidin-1-yl)ethanone derivatives 9(a-e) and 10(a-g) were synthesized and characterized by (1) H NMR, IR, mass spectral, and elemental analysis. These novel compounds were evaluated for their antileukemic activity against two human leukemic cell lines (K562 and CEM) by using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazoliumbromide assay. Some of the tested compounds showed good antiproliferative activity with IC(50) values ranging from 1.6 to 8.0 μm. Compound 9c, 9e, and 10f with an electron-withdrawing halogen substituent at the para position on the phenyl ring showed excellent in vitro potency against tested human leukemia cells (K562 and CEM).
一系列新型 2-(4-(2,4-二甲氧基苯甲酰基)苯氧基)-1-(4-(3-(哌啶-4-基)丙基)哌啶-1-基)乙酮衍生物 9(a-e)和 10(a-g)被合成并通过 (1) H NMR、IR、质谱和元素分析进行了表征。通过使用 3-(4,5-二甲基噻唑-2-基)-2,5-二苯基四氮唑溴盐测定法，这些新型化合物针对两种人白血病细胞系 (K562 和 CEM) 的抗白血病活性进行了评估。一些测试的化合物表现出良好的增殖抑制活性，IC(50) 值范围为 1.6 至 8.0 μm。在苯环的对位上带有吸电子卤素取代基的化合物 9c、9e 和 10f 对测试的人白血病细胞 (K562 和 CEM) 表现出优异的体外活性。
