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Antiproliferative activities of halogenated thieno[3,2-d]pyrimidines.
Temburnikar, Kartik W; Zimmermann, Sarah C; Kim, Nathaniel T; Ross, Christina R; Gelbmann, Christopher; Salomon, Christine E; Wilson, Gerald M; Balzarini, Jan; Seley-Radtke, Katherine L.
Afiliação
  • Temburnikar KW; Department of Chemistry and Biochemistry, University of Maryland Baltimore County, 1000 Hilltop Circle, Baltimore, MD 21250, USA.
  • Zimmermann SC; Department of Chemistry and Biochemistry, University of Maryland Baltimore County, 1000 Hilltop Circle, Baltimore, MD 21250, USA.
  • Kim NT; Department of Chemistry and Biochemistry, University of Maryland Baltimore County, 1000 Hilltop Circle, Baltimore, MD 21250, USA.
  • Ross CR; Department of Biochemistry and Molecular Biology, University of Maryland School of Medicine, 108 N. Greene Street, Baltimore, MD 21201, USA.
  • Gelbmann C; Center for Drug Design, University of Minnesota, 516 Delaware St. SE, Minneapolis, MN 55455, USA.
  • Salomon CE; Center for Drug Design, University of Minnesota, 516 Delaware St. SE, Minneapolis, MN 55455, USA.
  • Wilson GM; Department of Biochemistry and Molecular Biology, University of Maryland School of Medicine, 108 N. Greene Street, Baltimore, MD 21201, USA.
  • Balzarini J; Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat 10, B-3000 Leuven, Belgium.
  • Seley-Radtke KL; Department of Chemistry and Biochemistry, University of Maryland Baltimore County, 1000 Hilltop Circle, Baltimore, MD 21250, USA. Electronic address: kseley@umbc.edu.
Bioorg Med Chem ; 22(7): 2113-22, 2014 Apr 01.
Article em En | MEDLINE | ID: mdl-24631358
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.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Pirimidinas / Bacillus subtilis / Fungos / Antibacterianos / Antifúngicos / Antineoplásicos Limite: Humans Idioma: En Ano de publicação: 2014 Tipo de documento: Article

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Pirimidinas / Bacillus subtilis / Fungos / Antibacterianos / Antifúngicos / Antineoplásicos Limite: Humans Idioma: En Ano de publicação: 2014 Tipo de documento: Article