NDLI: A multi-target caffeine derived rhodium(I) N-heterocyclic carbene complex: evaluation of the mechanism of action

Content Provider	World Health Organization (WHO)-Global Index Medicus
Author	Schobert, Rainer Ott, Ingo Muenzner, Julienne K. Zhang, Jing-jing Abu El Maaty, Mohamed A. Karge, Bianka Wölfl, Stefan
Description	Author Affiliation: Zhang JJ ( Institute of Medicinal and Pharmaceutical Chemistry, Technische Universität Braunschweig, Beethovenstr. 55, D-38106 Braunschweig, Germany. ingo.ott@tu-bs.de and Institute of Pharmacy and Molecular Biotechnology, Ruprecht-Karls-Universität Heidelberg, Im Neuenheimer Feld 364, D-69120 Heidelberg, Germ); Muenzner JK ( Department of Organic Chemistry, University Bayreuth, Universitätsstr. 30, D-95440 Bayreuth, Germany.); Abu El Maaty MA ( Institute of Pharmacy and Molecular Biotechnology, Ruprecht-Karls-Universität Heidelberg, Im Neuenheimer Feld 364, D-69120 Heidelberg, Germany.); Karge B ( Department of Chemical Biology, Helmholtz Centre for Infection Research GmbH, Inhoffenstr. 7, D-38124 Braunschweig, Germany.); Schobert R ( Department of Organic Chemistry, University Bayreuth, Universitätsstr. 30, D-95440 Bayreuth, Germany.); Wölfl S ( Institute of Pharmacy and Molecular Biotechnology, Ruprecht-Karls-Universität Heidelberg, Im Neuenheimer Feld 364, D-69120 Heidelberg, Germany.); Ott I ( Institute of Medicinal and Pharmaceutical Chemistry, Technische Universität Braunschweig, Beethovenstr. 55, D-38106 Braunschweig, Germany. ingo.ott@tu-bs.de.)
Abstract	A rhodium(I) and a ruthenium(II) complex with a caffeine derived N-heterocyclic carbene (NHC) ligand were biologically investigated as organometallic conjugates consisting of a metal center and a naturally occurring moiety. While the ruthenium(II) complex was largely inactive, the rhodium(I) NHC complex displayed selective cytotoxicity and significant anti-metastatic and in vivo anti-vascular activities and acted as both a mammalian and an E. coli thioredoxin reductase inhibitor. In HCT-116 cells it increased the reactive oxygen species level, leading to DNA damage, and it induced cell cycle arrest, decreased the mitochondrial membrane potential, and triggered apoptosis. This rhodium(I) NHC derivative thus represents a multi-target compound with promising anti-cancer potential.
ISSN	14779226
Issue Number	33
Journal	Dalton Trans.
Volume Number	45
e-ISSN	13645447
Language	English
Publisher	Royal Society of Chemistry
Publisher Date	2016-08-16
Publisher Place	Great Britain (UK)
Access Restriction	Subscribed
Subject Keyword	Chemistry
Content Type	Text
Resource Type	Article
Subject	Inorganic Chemistry

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