Synthesis of novel tetrandrine derivatives and their inhibition against NSCLC A549 cells

J Asian Nat Prod Res. 2018 Nov;20(11):1064-1074. doi: 10.1080/10286020.2018.1478817. Epub 2018 May 31.

Abstract

A series of novel tetrandrine (Tet) derivatives were synthesized through Suzuki -Miyaura reaction and evaluated for their cytotoxicity against human non-small cell lung carcinoma (NSCLC) A549 cells. Interestingly, most of derivatives showed similar cytotoxicity to Tet against NSCLC A549 cells, and particularly, compounds Y5, Y6, Y9 and Y11 showed the most significant cytotoxic effects with IC50 values ranging from 3.87 to 4.66 mM. The present study is expected to contribute to the future design of more effective anticancer agents in lung cancer chemotherapy.

Keywords: NSCLC A549 cells; Suzuki-Miyaura reaction; Tetrandrine derivatives; anticancer activities; non-small cell lung carcinoma.

MeSH terms

  • A549 Cells
  • Antineoplastic Agents, Phytogenic / chemical synthesis
  • Antineoplastic Agents, Phytogenic / chemistry
  • Antineoplastic Agents, Phytogenic / pharmacology*
  • Benzylisoquinolines / chemistry*
  • Benzylisoquinolines / pharmacology*
  • Carcinoma, Non-Small-Cell Lung
  • Cell Survival / drug effects
  • Drug Screening Assays, Antitumor
  • Humans
  • Molecular Structure

Substances

  • Antineoplastic Agents, Phytogenic
  • Benzylisoquinolines
  • tetrandrine