Cancer preventive agents, Part 2: Synthesis and evaluation of 2-phenyl-4-quinolone and 9-oxo-9,10-dihydroacridine derivatives as novel antitumor promoters

Bioorg Med Chem. 2005 Jul 15;13(14):4396-401. doi: 10.1016/j.bmc.2005.04.078.

Abstract

2-Phenyl-4-quinolone and 9-oxo-9,10-dihydroacridine derivatives were synthesized and screened as potential antitumor promoters by examining the ability of the compounds to inhibit Epstein-Barr virus early antigen (EBV-EA) activation induced by the tumor promoter 12-O-tetradecanoylphorbol-13-acetate (TPA) in Raji cells. Interestingly, compounds 14, 15, and 17 showed similar inhibitory effects (89-92%, 66-69%, and 24-29% at 1000, 500, and 100 mol ratio to TPA, respectively) against EBV-EA with potencies comparable to those of glycyrrhetic acid, a known natural antitumor-promoter.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Acridines / chemical synthesis*
  • Acridines / chemistry
  • Acridines / pharmacology*
  • Anticarcinogenic Agents / chemical synthesis*
  • Anticarcinogenic Agents / chemistry
  • Anticarcinogenic Agents / pharmacology*
  • Cell Line
  • Humans
  • Magnetic Resonance Spectroscopy
  • Quinolones / chemical synthesis*
  • Quinolones / chemistry
  • Quinolones / pharmacology*
  • Spectrometry, Mass, Electrospray Ionization
  • Spectrophotometry, Infrared
  • Tetradecanoylphorbol Acetate / pharmacology

Substances

  • 9-oxo-9,10-dihydroacridine
  • Acridines
  • Anticarcinogenic Agents
  • Quinolones
  • 2-phenyl-4-oxohydroquinoline
  • Tetradecanoylphorbol Acetate