2. Academic Validation
  3. Synthesis and anti-proliferation activity of mogrol derivatives bearing quinoline and triazole moieties

Synthesis and anti-proliferation activity of mogrol derivatives bearing quinoline and triazole moieties

  • Bioorg Med Chem Lett. 2021 Jun 15:42:128090. doi: 10.1016/j.bmcl.2021.128090.
Jing-Ru Song 1,  Na Li 2,  Dian-Peng Li 3
Affiliations

Affiliations

  • 1 Guangxi Key Laboratory of Functional Phytochemicals Research and Utilization, Guangxi Institute of Botany, Chinese Academy of Sciences, Guilin 541006, China. Electronic address: songjingru@iccas.ac.cn.
  • 2 Guangxi Key Laboratory of Functional Phytochemicals Research and Utilization, Guangxi Institute of Botany, Chinese Academy of Sciences, Guilin 541006, China.
  • 3 Guangxi Key Laboratory of Functional Phytochemicals Research and Utilization, Guangxi Institute of Botany, Chinese Academy of Sciences, Guilin 541006, China. Electronic address: ldp@gxib.cn.
PMID: 33964443 DOI: 10.1016/j.bmcl.2021.128090
Abstract

A series of novel derivatives based on mogrol were designed and synthesized in attempt to improve anti-lung Cancer activity. The cytotoxicity against human lung Cancer cells including A549 and NCI-H460 were performed by Cell Counting Kit-8 (CCK8) assay in vitro. The screening result showed that compound 8f exhibited the strongest activity with an IC50 value of 4.47 μM against A549 cell, and could induce the cell Apoptosis in a dose-dependent manner and arrest cell cycle at G0/G1 phase. Besides, compound 8f displayed anti-proliferation effect on A549 cell through inhibiting phosphorylation of signal transducer and activator of transcription 3 (STAT3). Furthermore, compared with morgol, compound 10a significantly improved the cytotoxicity against NCI-H460 with the IC50 value of 17.13 μM. The research stimulated the development of potential therapeutic agent for lung Cancer from the natural mogrol.

Keywords

Lung cancer; Mogrol; Quinoline; Structural modification; Triazole.

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