Viral integrase (IN) enzymes such as HIV-IN and HTLV-IN (human T-cell leukemia virus integrase) are key enzymes involved in viral replication and are therefore attractive targets for development of antiviral chemotherapeutic agents. The active site of HIV-IN is well characterized and X-ray crystal structures of the catalytic domain allow structure-based drug design via virtual library screening (ligand docking) and traditional medicinal chemistry approaches. Here, we describe the synthesis of a small library of adenosine derivatives whose structures were indicated by docking an approximately 50,000-member virtual library (FLEXX, Sybyl 6.9, Tripos, Inc.) against the active site of HIV-IN (crystal structure 1BIU, Protein Databank). The synthetic library consisted of adenosine analogues 2 readily prepared from 3'-C functionalized adenosine derivative 1. Synthetic details and preliminary biological data will be presented.