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


ABSTRACT: [(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.

SUBMITTER: Lengacher R 

PROVIDER: S-EPMC8658909 | biostudies-literature | 2021 Dec

REPOSITORIES: biostudies-literature

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

Lengacher Raphael R   Wang Youchao Y   Braband Henrik H   Blacque Olivier O   Gasser Gilles G   Alberto Roger R  

Chemical communications (Cambridge, England) 20211209 98


[(η5-Cp)Re<sup>I</sup>(CO)<sub>3</sub>] 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 IC<sub>50</sub> value for the kinase SK2 is 30x higher than that of Opaganib®. The 99mTc homologue was synthesized, completing a matched-pair for molecular theranostics. ...[more]

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