Antiproliferative activities of halogenated thieno[3,2-d]pyrimidines

Kartik W. Temburnikar, Sarah C. Zimmermann, Nathaniel T. Kim, Christina R. Ross, Christopher Gelbmann, Christine E. Salomon, Gerald M. Wilson, Jan Balzarini, Katherine L. Seley-Radtke

Research output: Contribution to journalArticle

Abstract

The in vitro evaluation of thieno[3,2-d]pyrimidines identified halogenated compounds 1 and 2 with antiproliferative activity against three different cancer cell lines. A structure activity relationship study indicated the necessity of the chlorine at the C4-position for biological activity. The two most active compounds 1 and 2 were found to induce apoptosis in the leukemia L1210 cell line. Additionally, the compounds were screened against a variety of other microbial targets and as a result, selective activity against several fungi was also observed. The synthesis and preliminary biological results are reported herein.

Original languageEnglish (US)
Pages (from-to)2113-2122
Number of pages10
JournalBioorganic and Medicinal Chemistry
Volume22
Issue number7
DOIs
StatePublished - Apr 1 2014

Keywords

  • Antifungal
  • Apoptosis
  • Cytostatic
  • Heterocyclic chemistry
  • Thieno[3,2-d]pyrimidine

ASJC Scopus subject areas

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

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  • Cite this

    Temburnikar, K. W., Zimmermann, S. C., Kim, N. T., Ross, C. R., Gelbmann, C., Salomon, C. E., Wilson, G. M., Balzarini, J., & Seley-Radtke, K. L. (2014). Antiproliferative activities of halogenated thieno[3,2-d]pyrimidines. Bioorganic and Medicinal Chemistry, 22(7), 2113-2122. https://doi.org/10.1016/j.bmc.2014.02.033