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

Abstract

[(η5-Cp)Re^I(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.