Combined with an effective copper-catalyzed triazole-forming reaction,a series of novel camptothecin derivatives were synthesized. Incorporating oligo(ethylene glycol) chains into the derivatives enhanced their water-solubility when compared to the parent compound (up to 55-fold). Incorporating oligo (ethylene glycol) chains into the derivatives that enhance their water-solubility when compared to the parent compound (up to 55-fold).