Multi-target-directed design, syntheses, and characterization of fluorescent bisphosphonate derivatives as multifunctional enzyme inhibitors in mevalonate pathway

► Enzymes MVK, PMK, MDD, and FPPS, play regulatory roles in mevalonate pathway. ► Two fluorescent bisphosphonates were synthesized as multi-enzyme inhibitors. ► These two compounds had potent inhibition to all four enzymes. ► Kinetic and molecular modeling studies of these two compounds were carried out. ► Fluorescence microscopy indicated that the compounds could get into cancer cells.