Novel BODIPY–estrone and BODIPY–estradiol conjugates have been synthesized via Cu(I)- catalyzed azide-alkyne click (CuAAC) and/or Sonogashira reactions by selecting position C3-O for labeling. The steroidal azides and/or bromides were reacted with BODIPY-based fluorescent dye bearing alkyne function. The new fluorescent estrone conjugates might replace radiolabeled compounds in certain biochemical assays