Subtle Structural Changes across the Boundary between AR/AR Dual Antagonism and AR Antagonism: A Novel Class of 2-Aminopyrimidine-Based Derivatives.

Aberrantly elevated adenosine in the tumor microenvironment exerts its immunosuppressive functions through adenosine receptors AR and AR. Antagonism of AR and AR has the potential to suppress tumor growth. Herein, we report a systemic assessment of the effects of an indole modification at position 4, 5, 6, or 7 on both AR/AR activity and selectivity of novel 2-aminopyrimidine compounds.