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

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

  • Bioorg Med Chem. 2014 Apr 1;22(7):2113-22. doi: 10.1016/j.bmc.2014.02.033.
Kartik W Temburnikar 1,  Sarah C Zimmermann 1,  Nathaniel T Kim 1,  Christina R Ross 2,  Christopher Gelbmann 3,  Christine E Salomon 3,  Gerald M Wilson 2,  Jan Balzarini 4,  Katherine L Seley-Radtke 5
Affiliations

Affiliations

  • 1 Department of Chemistry and Biochemistry, University of Maryland Baltimore County, 1000 Hilltop Circle, Baltimore, MD 21250, USA.
  • 2 Department of Biochemistry and Molecular Biology, University of Maryland School of Medicine, 108 N. Greene Street, Baltimore, MD 21201, USA.
  • 3 Center for Drug Design, University of Minnesota, 516 Delaware St. SE, Minneapolis, MN 55455, USA.
  • 4 Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat 10, B-3000 Leuven, Belgium.
  • 5 Department of Chemistry and Biochemistry, University of Maryland Baltimore County, 1000 Hilltop Circle, Baltimore, MD 21250, USA. Electronic address: kseley@umbc.edu.
PMID: 24631358 DOI: 10.1016/j.bmc.2014.02.033
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.

Keywords

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

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