Gu Keli, Bi Lanrong, Zhao Ming, Wang Chao, Ju Jingfang, Peng Shiqi
College of Pharmaceutical Sciences, Capital University of Medical Sciences, Beijing 100054, PR China.
Bioorg Med Chem. 2007 Jul 15;15(14):4775-99. doi: 10.1016/j.bmc.2007.05.013. Epub 2007 May 6.
A new class of 2,5-disubstituted-dioxacycloalkanes were designed and synthesized via stereoselective synthetic method as cancer chemoprevention agents. The anti-inflammatory activities of these compounds were tested using the xylene-induced mouse ear edema model. Some of these compounds exhibited comparable or better anti-inflammatory activities than that of aspirin suggesting that they can be further developed as potential anti-inflammatory drug lead compounds. In addition, treatment of these anti-inflammatory agents did not prolong tail bleeding time in mice. The structure/activity relationships were also analyzed among these compounds.
通过立体选择性合成方法设计并合成了一类新型的2,5-二取代二氧杂环烷烃作为癌症化学预防剂。使用二甲苯诱导的小鼠耳肿胀模型测试了这些化合物的抗炎活性。其中一些化合物表现出与阿司匹林相当或更好的抗炎活性，这表明它们可以作为潜在的抗炎药物先导化合物进一步开发。此外，这些抗炎剂的处理并未延长小鼠的尾部出血时间。还分析了这些化合物之间的构效关系。
