摘要
本文以各种取代的靛红1、二烯酮3-烯基氧化吲哚2与脯氨酸或硫代脯氨酸,在有机溶剂乙腈中回流,进行1,3-偶极子3+2环加成反应,获得6个新型的姜黄酮骨架双螺环吡咯氧化吲哚类化合物(3a^3f,Scheme 1),产率65~81%,dr值10∶1~15∶1,其结构经~1H NMR,^(13)C NMR和HR-MS(ESI-TOF)表征。采用MTT法研究了3a^3f对人白血病细胞(K562)的体外抗肿瘤活性。结果表明:化合物3a对K562具有一定的抑制活性(IC50为27.9μM),接近于阳性对照药顺铂。
Six novel turmerone motif-fused 3,3'-pyrrolidinyl-dispirooxindoles( 3 a - 3 f) were synthesized via a multicomponent 1,3-dipolar cycloaddition event of dienones 2 with azomethine ylides( thermally generated in situ from isatins 1 and proline or thioproline). The yields and dr of 3 a - 3 f were 65% - 81% and 10 ∶1 - 15∶1,respectively. The structures were characterized by 1 H NMR,13 C NMR and HR-MS( ESI-TOF). The in vitro antitumor activities against human leukemia cells( K562) were demonstrated by MTT assays. The results showed that 3 a exhibited well inhibition activities against K562,showing IC50 27. 9 μM,and showed equipotent potent than the positive control of Cisplatin.
出处
《山地农业生物学报》
2017年第5期70-73,共4页
Journal of Mountain Agriculture and Biology
基金
国家自然科学基金资助项目(81660576
81603390)
贵州省教学改革创新项目(黔教研合JG字[2016]06)
贵州省中药民族药制药工程专业学位研究生工作站(黔教研合JYSZ字[2014]002)
贵州省药食两用资源应用开发工程实验室(黔发改投资[2015]542号)
贵州省高层次创新型人才培养(黔科合[2015]4032号)
贵州省药食同源资源研究开发科技创新人才团队(黔科合人才团队[2015]4010号)
贵州省药食同源植物资源开发工程技术研究中心(黔科合G字[2015]4001号)