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

Gengyang Yuan1, Tanner C Jankins1, Christopher G Patrick1

  • 1Department of Chemistry and Chemical Biology, Northeastern University, 360 Huntington Avenue, Boston, MA 02115, USA.

International Journal of Medicinal Chemistry
|December 5, 2017
PubMed

Insights

Blocking the adenosine A2A receptor on T cells can enhance anti-tumor immunity. Researchers identified preladenant and its derivatives, including compound 29, as promising immunotherapeutic agents for promoting tumor rejection.

Area of Science:

  • Immunology
  • Pharmacology
  • Oncology

Background:

  • The hypoxia-adenosinergic pathway can suppress anti-tumor immune responses.
  • Adenosine A2A receptors on T cells play a crucial role in this immunosuppression.

Purpose of the Study:

  • To investigate adenosine A2A receptor antagonists as a strategy to promote tumor rejection.
  • To identify novel immunotherapeutic agents targeting this pathway.

Main Methods:

  • Utilized an *in vivo* immunoassay with the Concanavalin A mouse model.
  • Employed molecular modeling for drug design and synthesis of analogs.
  • Conducted *in vitro* functional bioassays to evaluate compound efficacy.

Main Results:

  • Preladenant was identified as a potent lead compound.
  • Synthesized and evaluated various analogs, including PEGylated derivatives.
  • Compound 29, a fluorinated triethylene glycol derivative of preladenant, demonstrated significant potential.

Conclusions:

  • Antagonism of the adenosine A2A receptor effectively blocks the hypoxia-adenosinergic immunosuppressive pathway.
  • Compound 29 shows promise as a novel immunotherapeutic agent for cancer treatment.

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