济沅旋覆花 A 的 1,2,3-三唑衍生物的设计、合成及生物机制研究。
Design, synthesis and biological mechanisms research on 1,2,3-triazole derivatives of Jiyuan Oridonin A.
机构信息
Collaborative Innovation Center of New Drug Research and Safety Evaluation, Henan Province, Key Laboratory of Technology of Drug Preparation (Zhengzhou University), Ministry of Education of China, Key Laboratory of Henan Province for Drug Quality and Evaluation, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China.
Department of Pharmacy, Xuchang Central Hostipal, Xuchang 461000, China.
出版信息
Bioorg Med Chem. 2018 Sep 15;26(17):4761-4773. doi: 10.1016/j.bmc.2017.11.005. Epub 2017 Nov 4.
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.
两个系列的衍生物，以 1,2,3-三唑为杂环部分的济源冬凌草甲素，一种从冬凌草属中分离得到的新的贝壳杉烯二萜，被合成并进行了生物学评价。所有的衍生物都具有良好的抗增殖活性。其中，化合物 8g 通过一系列由增加的细胞内 ROS 水平激活的信号，显著诱导 MGC-803 细胞凋亡和细胞周期停滞。
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