Synthesis and evaluation of 2,7-diamino-thiazolo[4,5-d] pyrimidine analogues as anti-tumor epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors

Ronghui Lin, Sigmond G. Johnson, Peter J. Connolly, Steven K. Wetter, Eva Binnun, Terry V. Hughes, William V. Murray, Niranjan B. Pandey, Sandra J. Moreno-Mazza, Mary Adams, Angel R. Fuentes-Pesquera, Steven A. Middleton

Research output: Contribution to journalArticle

Abstract

2,7-Diamino-thiazolo[4,5-d]pyrimidine analogues were synthesized as novel epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors. Representative compounds showed potent and selective EGFR inhibitory activities and inhibited in vitro cellular proliferation in EGFR-overexpressing human tumor cells. The synthesis and preliminary biological, physical, and pharmacokinetic evaluation of these thiazolopyrimidine compounds are reported.

Original languageEnglish (US)
Pages (from-to)2333-2337
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume19
Issue number8
DOIs
StatePublished - Apr 15 2009
Externally publishedYes

Keywords

  • 2,7-Diamino-thiazolo[4,5-d]pyrimidine analogues
  • EGFR inhibitors
  • Epidermal growth factor receptor tyrosine kinase inhibitors

ASJC Scopus subject areas

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

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  • Cite this

    Lin, R., Johnson, S. G., Connolly, P. J., Wetter, S. K., Binnun, E., Hughes, T. V., Murray, W. V., Pandey, N. B., Moreno-Mazza, S. J., Adams, M., Fuentes-Pesquera, A. R., & Middleton, S. A. (2009). Synthesis and evaluation of 2,7-diamino-thiazolo[4,5-d] pyrimidine analogues as anti-tumor epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors. Bioorganic and Medicinal Chemistry Letters, 19(8), 2333-2337. https://doi.org/10.1016/j.bmcl.2009.02.067