Design and Evaluation of Xanthine Based Adenosine Receptor Antagonists: Potential Hypoxia Targeted Immunotherapies

Overview

Journal Bioorg Med Chem

Specialties Biochemistry
Chemistry

Date 2013 Oct 16

PMID 24126093

Citations 3

Authors

Rhiannon Thomas

Joslynn Lee

Vincent Chevalier

Sara Sadler

Kaisa Selesniemi

Stephen Hatfield

Michail Sitkovsky

Mary Jo Ondrechen

Graham B Jones

Affiliations

Soon will be listed here.

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.

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