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

Bioorg Med Chem. 2018 Sep 15;26(17):4761-4773. doi: 10.1016/j.bmc.2017.11.005.

Yu Ke ¹, Wang Wang ¹, Long-Fei Zhao ¹, Jian-Jia Liang ¹, Ying Liu ¹, Xiao Zhang ², Kai Feng ³, Hong-Min Liu ⁴

Affiliations

1 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.
2 Department of Pharmacy, Xuchang Central Hostipal, Xuchang 461000, China. Electronic address: [email protected].
3 Department of Pharmacy Administration, Shangqiu Central Hostipal, Shangqiu 476000, China. Electronic address: [email protected].
4 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. Electronic address: [email protected].

PMID: 30143365 DOI: 10.1016/j.bmc.2017.11.005

Abstract

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.

Keywords

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

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