Bis-MPA Janus dendrimers-prednisone conjugates against human breast cancer cells.

In this paper, we report the synthesis of Janus dendrimers using 2,2-bis(hydroxymethyl)propionic acid (bis-MPA) polyester dendrons with an azide and an alkyne group. The Janus dendrimers were obtained via azide-alkyne click reaction. The dendron and Janus dendrimers are shown to be selective against K-562 and MFC-7 cell lines. We found that the cytotoxic activity and selectivity against cancer cells of Janus prednisone-dendrimers depend on the functional groups in the dendritic arms. The conjugated dendrimer with OH as terminal groups was lower in activity against K-562 (IC50 38.98 ± 0.1  μM) than the Janus dendrimer with acetonide groups (IC50 28.87 ± 0.3  μM). Also, it was observed that the presence of the acetonide groups resulted in increased selectivity and cytotoxicity activity against MFC-7 (IC50 24.18 ± 0.4  μM). All the compounds studied showed no activity against normal cells. Our results suggest that polyethylene glycol and polyesters attached with prednisone in the dendrimer increase the bioavailability of the Janus dendrimer as an anticancer drug.