Ruthenacarborane-Phenanthroline Derivatives as Potential Metallodrugs.

Martin Kellert,Peter Lönnecke,Eric Meggers,Rajathees Rajaratnam,Evamarie Hey-Hawkins,Imola Sárosi

doi:10.3390/molecules25102322

Martin Kellert, Peter Lönnecke + Show 4 more

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https://doi.org/10.3390/molecules25102322

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Abstract

Ruthenium-based complexes have received much interest as potential metallodrugs. In this work, four RuII complexes bearing a dicarbollide moiety, a carbonyl ligand, and a phenanthroline-based ligand were synthesized and characterized, including single crystal diffraction analysis of compounds 2, 4, and 5 and an observed side product SP1. Complexes 2–5 are air and moisture stable under ambient conditions. They show excellent solubility in organic solvents, but low solubility in water.

Highlights

Metal-containing compounds are of increasing interest for applications in medicinal chemistry due to their diverse coordination geometries, unusual reactivities, and useful physicochemical properties [1,2,3]
Recently reported an interesting class of organometallic protein kinase inhibitors which were inspired by the alkaloid staurosporine (Figure 1) [4,15,16]
The ruthenium half-sandwich complex DW12 is a potent inhibitor of glycogen synthase kinase 3 (GSK-3), whereas staurosporine constitutes a very unselective inhibitor of a large number of protein kinases [5,16,17,18]

Summary

Introduction

Metal-containing compounds are of increasing interest for applications in medicinal chemistry due to their diverse coordination geometries, unusual reactivities, and useful physicochemical properties [1,2,3]. Ruthenium shows a low general toxicity [4] and is an excellent metal for this approach. The reactivity of ruthenium ions is well-known; reactions are predictable and facilitate drug design [5,6,7,8]. Predominantly ruthenium half-sandwich complexes have been developed as potential anti-cancer agents, antiproliferative drugs, antibiotics, and immunosuppressants [9,10,11,12,13,14]. Recently reported an interesting class of organometallic protein kinase inhibitors which were inspired by the alkaloid staurosporine (Figure 1) [4,15,16]. The ruthenium half-sandwich complex DW12 is a potent inhibitor of glycogen synthase kinase 3

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