Design and synthesis of 4β-Acetamidobenzofuranone-podophyllotoxin hybrids and their anti-cancer evaluation

Bioorg Med Chem Lett. 2019 Aug 15;29(16):2153-2156. doi: 10.1016/j.bmcl.2019.06.060. Epub 2019 Jun 29.

Abstract

A new series of amide derivatives of 4β-Acetamidobenzofuranone-podophyllotoxin hybrids (14a-g) were synthesized and their chemical structures were confirmed by 1H, 13C NMR and mass spectral data. Further, all the synthesized Acetamidobenzofuranone-podophyllotoxin hybrids were evaluated for in vitro cytotoxic activity against a panel of four human cancer cell lines i.e., human breast (MCF-7, MDA MB-231), lung (A549), and prostrate (DU-145). Among benzofuranone-podophyllotoxin hybrid compounds, 14b and 14e were exhibited more potent activity than standard drug and 14c and 14f were showed anticancer activity equivalent to etoposide.

Keywords: Acetamidobenzofuranone; Anti-cancer activity; Benzofuranone-podophyllotoxin hybrids; Etoposide; Teniposide.

Publication types

  • Letter
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents / therapeutic use*
  • Humans
  • Molecular Structure
  • Neoplasms / drug therapy*
  • Podophyllotoxin / chemical synthesis*
  • Podophyllotoxin / chemistry
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Podophyllotoxin