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Design, synthesis and biological mechanisms research on 1,2,3-triazole derivatives of Jiyuan Oridonin A
Bioorganic & Medicinal Chemistry ( IF 3.3 ) Pub Date : 2017-11-04 , DOI: 10.1016/j.bmc.2017.11.005 Yu Ke , Wang Wang , Long-Fei Zhao , Jian-Jia Liang , Ying Liu , Xiao Zhang , Kai Feng , Hong-Min Liu
中文翻译:
济源冬凌草甲素1,2,3-三唑衍生物的设计,合成及生物学机理研究
更新日期:2017-11-04
Bioorganic & Medicinal Chemistry ( IF 3.3 ) Pub Date : 2017-11-04 , DOI: 10.1016/j.bmc.2017.11.005 Yu Ke , Wang Wang , Long-Fei Zhao , Jian-Jia Liang , Ying Liu , Xiao Zhang , Kai Feng , Hong-Min Liu
Two series of derivatives with 1,2,3-triazole as heterocyclic moiety of Jiyuan Oridonin A, a new ent-kaurene diterpenoid which was isolated from genus Isodon rubescens, were synthesized and biologically evaluated. All the derivatives possessed good anti-proliferative activities. Among them, compound 8g was found to significantly induce cell apoptosis and cell cycle arrest in MGC-803 via a series of signals activated by the increased intracellular ROS levels.
中文翻译:
济源冬凌草甲素1,2,3-三唑衍生物的设计,合成及生物学机理研究
合成了由1,2,3-三唑作为济元冬凌草甲素A的杂环部分的两类衍生物,该衍生物是从红冬凌草(Isodon rubescens)属中分离得到的一种新的对映体-月桂烯二萜类化合物。所有衍生物均具有良好的抗增殖活性。其中,发现化合物8g通过一系列由细胞内ROS水平升高激活的信号显着诱导MGC-803中的细胞凋亡和细胞周期停滞。