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Fluorinated Adenosine A2A Receptor Antagonists Inspired by Preladenant as Potential Cancer Immunotherapeutics.

ABSTRACT: Antagonism of the adenosine A2A receptor on T cells blocks the hypoxia-adenosinergic pathway to promote tumor rejection. Using an in vivo immunoassay based on the Concanavalin A mouse model, a series of A2A antagonists were studied and identified preladenant as a potent lead compound for development. Molecular modeling was employed to assist drug design and subsequent synthesis of analogs and those of tozadenant, including fluorinated polyethylene glycol PEGylated derivatives. The efficacy of the analogs was evaluated using two in vitro functional bioassays, and compound 29, a fluorinated triethylene glycol derivative of preladenant, was confirmed as a potential immunotherapeutic agent.

SUBMITTER: Yuan G 

PROVIDER: S-EPMC5671725 | biostudies-literature | 2017

REPOSITORIES: biostudies-literature

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Fluorinated Adenosine A<sub>2A</sub> Receptor Antagonists Inspired by Preladenant as Potential Cancer Immunotherapeutics.

Yuan Gengyang G   Jankins Tanner C TC   Patrick Christopher G CG   Philbrook Phaethon P   Sears Olivia O   Hatfield Stephen S   Sitkovsky Michail M   Vasdev Neil N   Liang Steven H SH   Ondrechen Mary Jo MJ   Pollastri Michael P MP   Jones Graham B GB  

International journal of medicinal chemistry 20171019

Antagonism of the adenosine A<sub>2A</sub> receptor on T cells blocks the hypoxia-adenosinergic pathway to promote tumor rejection. Using an <i>in vivo</i> immunoassay based on the Concanavalin A mouse model, a series of A<sub>2A</sub> antagonists were studied and identified preladenant as a potent lead compound for development. Molecular modeling was employed to assist drug design and subsequent synthesis of analogs and those of tozadenant, including fluorinated polyethylene glycol PEGylated de  ...[more]

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