A novel 5-[1,3,4-oxadiazol-2-yl]-N-aryl-4,6-pyrimidine diamine having dual EGFR/HER2 kinase activity: Design, synthesis, and biological activity

Terry V. Hughes, Guozhang Xu, Steven K. Wetter, Peter J. Connolly, Stuart L. Emanuel, Prabha Karnachi, Scott R. Pollack, Niranjan Pandey, Mary Adams, Sandra Moreno-Mazza, Steven A. Middleton, Lee M. Greenberger

Research output: Contribution to journalArticle

Abstract

A novel 5-[1,3,4-oxadiazol-2-yl]-N-aryl-4,6-pyrimidine diamine was synthesized and found to have potent dual EGFR/HER2 kinase inhibitory activity. The structure-based drug design of this molecule as well as the kinase and cellular inhibition of HER2 kinase dependent cell lines will be discussed.

Original languageEnglish (US)
Pages (from-to)4896-4899
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume18
Issue number17
DOIs
StatePublished - Sep 1 2008
Externally publishedYes

Keywords

  • EGFR
  • HER1
  • HER2
  • Intramolecular hydrogen bond
  • Kinase
  • Oxadiazole
  • Pyrimidine
  • Quinazoline mimic
  • Restricted rotation

ASJC Scopus subject areas

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

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    Hughes, T. V., Xu, G., Wetter, S. K., Connolly, P. J., Emanuel, S. L., Karnachi, P., Pollack, S. R., Pandey, N., Adams, M., Moreno-Mazza, S., Middleton, S. A., & Greenberger, L. M. (2008). A novel 5-[1,3,4-oxadiazol-2-yl]-N-aryl-4,6-pyrimidine diamine having dual EGFR/HER2 kinase activity: Design, synthesis, and biological activity. Bioorganic and Medicinal Chemistry Letters, 18(17), 4896-4899. https://doi.org/10.1016/j.bmcl.2008.07.057