Design, synthesis, and antiproliferative activity of some novel aminosubstituted xanthenones, able to overcome multidrug resistance toward MES-SA/Dx5 cells

Bioorg Med Chem Lett. 2005 Nov 15;15(22):5057-60. doi: 10.1016/j.bmcl.2005.07.079.

Abstract

A series of novel xanthenone aminoderivatives and their pyrazole-fused counterparts possessing structural analogy to the potent anticancer agent 9-methoxypyrazoloacridine (PZA) reported. These compounds exhibited an interesting cytotoxic activity against a panel of cell lines. Most noticeably, they retain activity against the multidrug resistant MES-SA/Dx5 subline, showing resistant factors close to 1.

MeSH terms

  • Amination
  • Animals
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Drug Design*
  • Drug Resistance, Multiple / drug effects*
  • Humans
  • Inhibitory Concentration 50
  • Mice
  • Molecular Structure
  • Pyrazoles / chemistry
  • Xanthenes / chemical synthesis
  • Xanthenes / chemistry*
  • Xanthenes / pharmacology*

Substances

  • Pyrazoles
  • Xanthenes
  • pyrazole