Synthesis and in vitro antitumor evaluation of honokiol derivatives

Bioorg Med Chem Lett. 2020 Jan 15;30(2):126849. doi: 10.1016/j.bmcl.2019.126849. Epub 2019 Dec 3.

Abstract

Honokiol is a natural bioactive neolignan and has been widely researched and structural modified as an anticancer agent. In this paper, 18 honokiol derivatives were synthesized and investigated for their antitumor activity. Among these, the promising compound 5a exhibited much higher anti-proliferative activity with IC50 value of 10.41 μM. Transwell assays showed that 5a could significantly inhibit the invasion and migration of I-10 cells at 2.5 μM, which was further confirmed by the western blotting experiments with down-regulation of the HIF-1α and its associated downstream proteins MMP-2 and MMP-9. Overall, these results provided useful suggestion for further structural optimization of honokiol derivatives.

Keywords: Cytotoxicity; Honokiol derivatives; Invasion; Migration.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents / therapeutic use*
  • Biphenyl Compounds / chemical synthesis*
  • Biphenyl Compounds / chemistry
  • Humans
  • Lignans / chemical synthesis*
  • Lignans / chemistry
  • Neoplasms / drug therapy*

Substances

  • Antineoplastic Agents
  • Biphenyl Compounds
  • Lignans
  • honokiol