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

Raphael Lengacher; Youchao Wang; Henrik Braband; Olivier Blacque; Gilles Gasser; Roger Alberto

doi:10.1039/d1cc03678e

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

Chem Commun (Camb). 2021 Dec 9;57(98):13349-13352. doi: 10.1039/d1cc03678e.

Authors

Raphael Lengacher¹, Youchao Wang², Henrik Braband¹, Olivier Blacque¹, Gilles Gasser², Roger Alberto¹

Affiliations

¹ University of Zurich, Department of Chemistry, Zurich, Switzerland. [email protected].
² Chimie ParisTech, PSL University, CNRS, Institute of Chemistry for Life and Health Sciences, Laboratory for Inorganic Chemical Biology, Paris F-75005, France.

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.