Aqueous Compatible Fullerene-Doxorubicin Conjugates.

ABSTRACT

Covalent conjugates of fullerene C(60) and the highly effective anticancer drug doxorubicin (DOX) were prepared and studied. The conjugation was through the amide linkage to preserve the intrinsic properties of DOX and fullerene cage. As designed, the conjugates with hydrophilic ethylene glycol spacers exhibited much improved aqueous compatibility, with significant solubility in water-DMSO mixtures. The anti-neoplastic activities of DOX were apparently unaffected in the conjugates according to evaluations in vitro with a human breast cancer cell line.