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Bioorg Med Chem. 2013 Dec 1;21(23):7453-64. doi: 10.1016/j.bmc.2013.09.043. Epub 2013 Sep 28.

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

Author information

1
Bioorganic and Medicinal Chemistry Laboratories, Department of Chemistry and Chemical Biology, Northeastern University, 360 Huntington Avenue, Boston, MA 02115, United States.

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.

KEYWORDS:

A(2A); Adenosine receptor; Hypoxia; KW-6002; Synthesis; Xanthine

PMID:
24126093
PMCID:
PMC4346301
DOI:
10.1016/j.bmc.2013.09.043
[Indexed for MEDLINE]
Free PMC Article

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