[Development of Bio-active Fullerene Derivatives Suitable for Drug]

Fullerene (C₆₀) and fullerene derivatives are attractive novel compounds not only for carbon materials of nanotechnology but also for medical fields because of its unique chemical and physical properties. We intend to develop fullerene derivatives as novel lead compounds for drug discovery. At first, we synthesized many types of water-soluble fullerene derivatives to investigate their biological activities because of their poor solubility in water. We found that anionic fullerene derivatives possess anti-oxidant activities, whereas di-cationic fullerene derivatives exhibited antiproliferative activities against various cancer cell lines including drug-resistant cells. Proline-type fullerene derivatives showed inhibitory activities against human immunodeficiency virus (HIV) reverse transcriptase, HIV protease, hepatitis C virus (HCV) NS5B RNA polymerase, and HCV NS3/4A protease. These activities may strongly inhibit virus replication via a synergistic effect and fullerene derivatives may be used as novel multi-target drugs for the treatment of AIDS and hepatitis C in the future.