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

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.

SUBMITTER: Thomas R 

PROVIDER: S-EPMC4346301 | biostudies-literature | 2013 Dec

REPOSITORIES: biostudies-literature