Abstract Human A 3 adenosine receptor (hA 3 AR) is a membrane-bound G protein-coupled receptor implicated in a number of severe pathological conditions, including cancer, in which it acts as a potential therapeutic target. To derive structure–activity relationships on pyrazolo–triazolo–pyrimidine (PTP)-based A 3 AR antagonists, we developed a new class of organometallic inhibitors through replacement of the triazolo moiety with an ...