Abstract Melanoma is a highly aggressive cancer with limited therapeutic options. In melanoma cell lines, β 2 AR activation leads to the suppression of pro-proliferatory MAPK/ERK signaling. This suggests that fenoterol, a potent β 2 AR agonist, can be useful in the treatment of melanoma. Here, we investigated the structure–activity relationship (SAR) of fenoterol derivatives for β 2 AR-depedent ERK suppression. We used the UACC-647 human-derived melanoma cell line to screen a panel of chiral com