Adenosine is an endogenous purine-based nucleoside expressed nearly in all body tissues.
It regulates various body functions by activating four G-protein coupled receptors, A 1, A 2A …

Dihydroazolopyrimidines are an important class of heterocycles that are isosteric to natural
purines and are therefore of great interest primarily as drug‐like molecules. In contrast to the …

The modulation of the A2B adenosine receptor is a promising strategy in cancer (immuno)
therapy, with A2BAR antagonists emerging as immune checkpoint inhibitors. Herein, we …

We present and thoroughly characterize a large collection of 3, 4-dihydropyrimidin-2 (1 H)-
ones as A2BAR antagonists, an emerging strategy in cancer (immuno) therapy. Most …

The four adenosine receptors (ARs) A1AR, A2AAR, A2BAR, and A3AR are G protein-
coupled receptors (GPCRs) for which an exceptional amount of experimental and structural …

A systematic exploration of bioisosteric replacements for furan and thiophene cores in a
series of potent A2BAR antagonists has been carried out using the nitrogen-walk approach …

Abstract An efficient and practical 1, 3‐dipolar [3+ 2] cycloaddition of N‐2, 2, 2‐
trifluoroethylisatin ketimines and maleimides has been achieved through phase‐transfer …

Antagonists of the A 2B adenosine receptor have recently emerged as targeted anticancer
agents and immune checkpoint inhibitors within the realm of cancer immunotherapy. This …

G-protein coupled receptors (GPCRs) have been largely targeted in a wide range of
diseases, but few therapies have been directed against GPCRs in the field of cancer, partly …

We herein document a large collection of 108 2-amino-4, 6-disubstituted-pyrimidine
derivatives as potent, structurally simple, and highly selective A1AR ligands. The most …