Synthesis and screening of 3-substituted thioxanthen-9-one-10,10-dioxides

Bioorg Med Chem Lett. 2007 Nov 1;17(21):5940-3. doi: 10.1016/j.bmcl.2007.07.103. Epub 2007 Aug 25.

Abstract

This manuscript describes methods appropriate for the parallel synthesis of libraries based on the tricyclic thioxanthen-9-one-10,10-dioxide scaffold. The novel compounds were synthesized from previously reported 3-chlorothioxanthen-9-one-10,10-dioxide and commercially available 3-carboxylic acid thioxanthen-9-one-10,10-dioxide. The library members were screened for activity in a fluorescence polarization assay for inhibitors of BRCT domains of breast cancer gene 1 and in cell-based secreted alkaline phosphatase reported replicon system for activity against hepatitis C virus.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Antiviral Agents / chemical synthesis*
  • Antiviral Agents / pharmacology*
  • Fluorescence Polarization
  • Hepacivirus / drug effects
  • Xanthenes / chemical synthesis*
  • Xanthenes / pharmacology*

Substances

  • Antiviral Agents
  • Xanthenes