Starting soon after the production of fullerenes in 1990, many efforts have
been devoted to the application Of C-60 and its derivatives. In fact, [60]
fullerene possesses a variety of interesting biological properties, such as
HIV-P inhibition, DNA photocleavage, neuroprotection, apoptosis, etc. Unfo
rtunately, the low solubility in biological fluids limits the use of these
compounds as new pharmacophores for structure-activity relationship studies
in medicinal chemistry. This article briefly summarizes recent studies on
the functionalization Of C-60 aimed at increasing water solubility as well
as the preliminary studies performed on biological targets. In particular,
the HIV-P inhibition, DNA photocleavage and antibacterial activity are disc
ussed.