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 journalArticlepeer-review

23 Scopus citations

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

Bibliographical note

Funding Information:
This work was supported in part by the National Institutes of Health (R01GM073645 KSR). The authors are grateful to Robin Patel for the gift of the clinical isolates of C. neoformans . We also thank Yudi Rusman for his assistance with the antifungal dose response experiments.

Keywords

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

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