Synthesis of novel chemical probes for the study of tanshinone binding proteins.

Novel diazirine or biotin-labeled tanshinone probes were synthesized and evaluated for TRAP inhibitory activity against RANKL-induced osteoclastogenesis in RAW264.7 cells. We found that diazirine-labeled derivatives (18 and 20) are potent inhibitors of RANKL-induced osteoclastogenesis. IC50 values were 18.02 and 15.00 microM, respectively. These probes will be useful reagents for investigating tanshinone-proteins interactions.