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

  • Bioorg Med Chem Lett. 2006 Sep 15;16(18):4733-7. doi: 10.1016/j.bmcl.2006.07.019.
Jin-Soo Lee  1 ,  Sun-Young Han ,  Myong Sang Kim ,  Chan-Mo Yu ,  Myung Hee Kim ,  Seong Hwan Kim ,  Yong Ki Min ,  Bum Tae Kim
Affiliations
  • 1. Laboratory of Chemical Genomics, Bio-Organic Science Division, Korea Research Institute of Chemical Technology, Deajeon 305-600, Republic of Korea.
PMID: 16872829 DOI: 10.1016/j.bmcl.2006.07.019
Abstract

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.