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 Citations (Scopus)

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

Fingerprint

Libraries
Screening
Replicon
Fluorescence Polarization
Neoplasm Genes
Carboxylic Acids
Viruses
Scaffolds
Hepacivirus
Alkaline Phosphatase
Assays
Genes
Fluorescence
Polarization
Breast Neoplasms

Keywords

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

ASJC Scopus subject areas

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

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

Synthesis and screening of 3-substituted thioxanthen-9-one-10,10-dioxides. / Lory, Pedro M.J.; Estrella-Jimenez, Maria E.; Shashack, Matthew J.; Lokesh, Ganesh L.; Natarajan, Amarnath; Gilbertson, Scott R.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 17, No. 21, 01.11.2007, p. 5940-5943.

Research output: Contribution to journalArticle

Lory, PMJ, Estrella-Jimenez, ME, Shashack, MJ, Lokesh, GL, Natarajan, A & Gilbertson, SR 2007, 'Synthesis and screening of 3-substituted thioxanthen-9-one-10,10-dioxides', Bioorganic and Medicinal Chemistry Letters, vol. 17, no. 21, pp. 5940-5943. https://doi.org/10.1016/j.bmcl.2007.07.103
Lory, Pedro M.J. ; Estrella-Jimenez, Maria E. ; Shashack, Matthew J. ; Lokesh, Ganesh L. ; Natarajan, Amarnath ; Gilbertson, Scott R. / Synthesis and screening of 3-substituted thioxanthen-9-one-10,10-dioxides. In: Bioorganic and Medicinal Chemistry Letters. 2007 ; Vol. 17, No. 21. pp. 5940-5943.
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