Preparation of sulfonamido nucleosides as human adenosine A3 receptro agonists and antitumor agents.

The invention realizes that a series of sulfonamido derivs. I, wherein wherein Ar is an aryl group; and R and R1 are independently H, alkyl, aryl, heteroaryl, alkenyl, cycloalkenyl, cycloalkyl, alkoxy, alkynyl, and where taken together R and R1 may form a or carbocyclic or heterocyclic fused ring system which includes both alicyclic and arom. structures with a conserved uronamide group at the 5' position provide superior A3 receptor affinity as well as selectivity. These new adenosine agonists are sulfonamido derivs. N-substituted with aliph. groups (cyclic or linear) or arom. radicals. Mediation of the A3 receptor has been found to induce behavioral depression and protect against cerebral ischemia, and to induce apoptosis in HL-60 human leukemia cells. The A3 adenosine receptor is known to mediate many processes, such as inflammation, hypotension, and mast cell deregulation. These compds. can be used to treat cancer. This particularly includes cancers that express elevated levels of A3 receptors. This would include, but not be limited to, ovarian cancer, breast cancer, colon cancer, and melanoma. Thus, nucleoside II was prepd. and tested in vitro as adenosine A3 receptor agonist and antitumor agent.