Design and evaluation of xanthine based adenosine receptor antagonists: Potential hypoxia targeted immunotherapies

Rhiannon Thomas, Joslynn Lee, Vincent Chevalier, Sara Sadler, Kaisa Selesniemi, Stephen Hatfield, Michail Sitkovsky, Mary Jo Ondrechen, Graham B. Jones

Research output: Contribution to journalArticlepeer-review

9 Scopus citations

Abstract

Molecular modeling techniques were applied to the design, synthesis and optimization of a new series of xanthine based adenosine A2A receptor antagonists. The optimized lead compound was converted to a PEG derivative and a functional in vitro bioassay used to confirm efficacy. Additionally, the PEGylated version showed enhanced aqueous solubility and was inert to photoisomerization, a known limitation of existing antagonists of this class.

Original languageEnglish (US)
Pages (from-to)7453-7464
Number of pages12
JournalBioorganic and Medicinal Chemistry
Volume21
Issue number23
DOIs
StatePublished - Dec 1 2013

Keywords

  • A
  • Adenosine receptor
  • Hypoxia
  • KW-6002
  • Synthesis
  • Xanthine

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