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Organometallic small molecule kinase inhibitors - direct incorporation of Re and 99mTc into Opaganib®.

Raphael LengacherYouchao WangHenrik BrabandOlivier BlacqueGilles GasserRoger A Alberto
Published in: Chemical communications (Cambridge, England) (2021)
[(η5-Cp)ReI(CO)3] was incorporated into the kinase inhibitor Opaganib®. The resulting bioorganometallic complex showed a similar anti-cancer activity to Opaganib® against PC-3 cancer cells. The IC50 value for the kinase SK2 is 30x higher than that of Opaganib®. The 99mTc homologue was synthesized, completing a matched-pair for molecular theranostics.
Keyphrases
  • small molecule
  • protein protein
  • protein kinase
  • single molecule
  • oxide nanoparticles