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ID: ALA3091430
Journal: Bioorg Med Chem
Title: Design and evaluation of xanthine based adenosine receptor antagonists: potential hypoxia targeted immunotherapies.
Authors: Thomas R, Lee J, Chevalier V, Sadler S, Selesniemi K, Hatfield S, Sitkovsky M, Ondrechen MJ, Jones GB.
Abstract: Molecular modeling techniques were applied to the design, synthesis and optimization of a new series of xanthine based adenosine A(2A) 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.
CiteXplore: 24126093