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

Pedro M.J. Lory, Maria E. Estrella-Jimenez, Matthew J. Shashack, Ganesh L. Lokesh, Amarnath Natarajan, Scott R. Gilbertson

Research output: Contribution to journalArticle

6 Scopus citations

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.

Original languageEnglish (US)
Pages (from-to)5940-5943
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume17
Issue number21
DOIs
StatePublished - Nov 1 2007

Keywords

  • Amide
  • Amine
  • Microwave
  • Thioxanthen-9-one

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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  • Cite this

    Lory, P. M. J., Estrella-Jimenez, M. E., Shashack, M. J., Lokesh, G. L., Natarajan, A., & Gilbertson, S. R. (2007). Synthesis and screening of 3-substituted thioxanthen-9-one-10,10-dioxides. Bioorganic and Medicinal Chemistry Letters, 17(21), 5940-5943. https://doi.org/10.1016/j.bmcl.2007.07.103