Organometallic small molecule kinase inhibitors – direct incorporation of Re and (99m)Tc into Opaganib®

[(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 IC(50) value for the kinase SK2 is 30x higher than that of Opaganib®. The (99m)Tc homologue was synthe...

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Autores principales: Lengacher, Raphael, Wang, Youchao, Braband, Henrik, Blacque, Olivier, Gasser, Gilles, Alberto, Roger
Formato: Online Artículo Texto
Lenguaje:English
Publicado: The Royal Society of Chemistry 2021
Materias:
Chemistry
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8658909/
https://www.ncbi.nlm.nih.gov/pubmed/34817478
http://dx.doi.org/10.1039/d1cc03678e
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author Lengacher, Raphael
Wang, Youchao
Braband, Henrik
Blacque, Olivier
Gasser, Gilles
Alberto, Roger
author_facet Lengacher, Raphael
Wang, Youchao
Braband, Henrik
Blacque, Olivier
Gasser, Gilles
Alberto, Roger
author_sort Lengacher, Raphael
collection PubMed
description [(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 IC(50) value for the kinase SK2 is 30x higher than that of Opaganib®. The (99m)Tc homologue was synthesized, completing a matched-pair for molecular theranostics.
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spelling pubmed-86589092022-01-06 Organometallic small molecule kinase inhibitors – direct incorporation of Re and (99m)Tc into Opaganib® Lengacher, Raphael Wang, Youchao Braband, Henrik Blacque, Olivier Gasser, Gilles Alberto, Roger Chem Commun (Camb) Chemistry [(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 IC(50) value for the kinase SK2 is 30x higher than that of Opaganib®. The (99m)Tc homologue was synthesized, completing a matched-pair for molecular theranostics. The Royal Society of Chemistry 2021-11-20 /pmc/articles/PMC8658909/ /pubmed/34817478 http://dx.doi.org/10.1039/d1cc03678e Text en This journal is © The Royal Society of Chemistry https://creativecommons.org/licenses/by/3.0/
spellingShingle Chemistry
Lengacher, Raphael
Wang, Youchao
Braband, Henrik
Blacque, Olivier
Gasser, Gilles
Alberto, Roger
Organometallic small molecule kinase inhibitors – direct incorporation of Re and (99m)Tc into Opaganib®
title Organometallic small molecule kinase inhibitors – direct incorporation of Re and (99m)Tc into Opaganib®
title_full Organometallic small molecule kinase inhibitors – direct incorporation of Re and (99m)Tc into Opaganib®
title_fullStr Organometallic small molecule kinase inhibitors – direct incorporation of Re and (99m)Tc into Opaganib®
title_full_unstemmed Organometallic small molecule kinase inhibitors – direct incorporation of Re and (99m)Tc into Opaganib®
title_short Organometallic small molecule kinase inhibitors – direct incorporation of Re and (99m)Tc into Opaganib®
title_sort organometallic small molecule kinase inhibitors – direct incorporation of re and (99m)tc into opaganib®
topic Chemistry
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8658909/
https://www.ncbi.nlm.nih.gov/pubmed/34817478
http://dx.doi.org/10.1039/d1cc03678e
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