Al-Neyadi Shaikha S, Hassan Ahmed H, Abdou Ibrahim M
Department of Chemistry, Faculty of Science, United Arab Emirates University, Al-Ain, United Arab Emirates.
Nucleosides Nucleotides Nucleic Acids. 2011 Feb;30(2):120-34. doi: 10.1080/15257770.2010.551646.
A new series of substituted 2(1H)-pyridones (4a-i) and their glucosides (5, 6a-e) were prepared as potential agents against leukemia (HL-60) cells. Glucosides (5,6a-e) were synthesized using three independent methods. Microwave protocol as an ecologically new method was used to synthesize the target compounds. Structures of the new products were confirmed using one- and two-dimensional NMR spectroscopy. In vitro exposure of pyridones substituted at position 4 with a 2-thienyl or 2-(trifluoromethyl)phenyl were found to exhibit high antiproliferation activities; in particular, 3-cyano-4-(thien-2'-yl)-6-(4''-chlorophenyl)-2(1H)-pyridone (4c) and its glucoside analogue (6c) had the highest activity.
制备了一系列新型取代的2(1H)-吡啶酮(4a-i)及其糖苷(5,6a-e)，作为抗白血病(HL-60)细胞的潜在药物。糖苷(5,6a-e)采用三种独立方法合成。微波法作为一种生态新方法用于合成目标化合物。通过一维和二维核磁共振光谱确定了新产品的结构。发现4位被2-噻吩基或2-(三氟甲基)苯基取代的吡啶酮的体外暴露表现出高抗增殖活性；特别是，3-氰基-4-(噻吩-2'-基)-6-(4''-氯苯基)-2(1H)-吡啶酮(4c)及其糖苷类似物(6c)具有最高活性。
