节点文献
澳洲茄胺单糖苷的合成及其抗肿瘤活性
Synthesis and Antitumor Activities of Monoglycosides of Solasodine
【摘要】 以单糖为原料,经苯甲酰化保护和溴代制备中间体酰化溴代糖(3a~3e)。通过Koenigs-Knorr合成法将3a~3e与澳洲茄胺甙化缩合并脱保护合成了5个澳洲茄胺单糖苷化合物(5a~5e,5d和5e为新化合物),其结构经1H NMR,13C NMR和MS表征。用MTT法对5a~5e进行体外抗肿瘤细胞活性试验结果表明,5c和5d显示了较好的抗肿瘤活性。
【Abstract】 Five intermediates,benzoyl saccharides bromides(3a~3e),were prepared from monosaccharides by protection with benzoyl chloride and bromination.The monoglycosides(5a~5e,5d and 5e were new compounds) of solasodine were synthesized by glycosidation of 3a~3e with solasodine and deprotection.The structures were characterized by 1H NMR,13C NMR and MS.The in vitro antitumor activities of 5a~5e against some cancer cells were tested by the MTT method.The results showed that 5c and 5d exhibited better antitumor activities.
【关键词】 澳洲茄边碱;
澳洲茄胺;
糖甙化;
合成;
抗肿瘤活性;
【Key words】 solamargine; solasodine; glycosidation; synthesis; antitumor activity;
【Key words】 solamargine; solasodine; glycosidation; synthesis; antitumor activity;
【基金】 国家重大新药创制课题(2009ZX09103-359);上海市科委资助课题(09DZ1970200)
- 【文献出处】 合成化学 ,Chinese Journal of Synthetic Chemistry , 编辑部邮箱 ,2013年03期
- 【分类号】R284;R285
- 【被引频次】3
- 【下载频次】117