Design, synthesis and biological mechanisms research on 1,2,3-triazole derivatives of Jiyuan Oridonin A

作者：Ke, Yu; Wang, Wang; Zhao, Long-Fei; Liang, Jian-Jia; Liu, Ying; Zhang, Xiao^*; Feng, Kai^*; Liu, Hong-Min^*

来源：Bioorganic & Medicinal Chemistry, 2018, 26(17): 4761-4773.

DOI：10.1016/j.bmc.2017.11.005

• ent-Kaurene diterpenoid
• 1,2,3-Triazole
• MGC-803
• ROS

Two series of derivatives with 1,2,3-triazole as heterocyclic moiety of Jiyuan Oridonin A, a new entkaurene 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.

• 出版日期2018-9-15
• 单位郑州大学