Synthesis of water-soluble chlorambucil Janus dendrimers

In this paper we reported a new range of amphiphilic Janus dendrimers, which consist of sodium carboxylate and chlorambucil molecules as the peripheral groups, as novel potential anticancer dendritic drug delivery agents. The dendrons and structural features of the Janus dendrimers were analyzed by different techniques (¹H, ¹³C one- and two-dimension NMR spectroscopy, FTIR, UV–vis and mass spectrometry). The amphiphilic dendrimers were loaded with the water-insoluble anticancer drug, chlorambucil, by a covalent bond. The hydrophilic group, sodium carboxylate, was obtained from the Behera’s amine moieties. The Janus dendrimers take advantage of a dendritic display to carry different amounts of chlorambucil molecules. The Janus dendrimers chlorambucil-sodium-carboxylate as terminal groups were more active than its tert-butyl and OH substituted analogues against cancer cells. These results provide an effective entry to the development of new drug nanocarriers.