Synthesis and anticancer activity evaluation of η5-C5(CH3)4R ruthenium complexes bearing chelating diphosphine ligands

A. Rodríguez-Bárzano, R. M. Lord, A. M. Basri, R. M. Phillips, A. J. Blacker, P. C. McGowan

Research output: Contribution to journalArticle

6 Citations (Scopus)

Abstract

The complexes [RuCp∗(PP)Cl] (Cp∗ = C5Me5; [1], PP = dppm; [4], PP = Xantphos), [RuCp#(PP)Cl] (Cp# = C5Me4(CH2)5OH; [2], PP = dppm; [5], PP = Xantphos) and [RuCp∗(dppm)(CH3CN)][SbF6] [3] were synthesized and evaluated in vitro as anticancer agents. Compounds 1-3 gave nanomolar IC50 values against normoxic A2780 and HT-29 cell lines, and were also tested against hypoxic HT-29 cells, maintaining their high activity. Complex 3 yielded an IC50 value of 0.55 ± 0.03 μM under a 0.1% O2 concentration.

Original languageEnglish
Pages (from-to)3265-3270
Number of pages6
JournalDalton Transactions
Volume44
Issue number7
DOIs
Publication statusPublished - 5 Jan 2015
Externally publishedYes

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Bearings (structural)
HT29 Cells
Ruthenium
Chelation
Inhibitory Concentration 50
Ligands
Antineoplastic Agents
Cells
Cell Line
xantphos

Cite this

Rodríguez-Bárzano, A. ; Lord, R. M. ; Basri, A. M. ; Phillips, R. M. ; Blacker, A. J. ; McGowan, P. C. / Synthesis and anticancer activity evaluation of η5-C5(CH3)4R ruthenium complexes bearing chelating diphosphine ligands. In: Dalton Transactions. 2015 ; Vol. 44, No. 7. pp. 3265-3270.
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abstract = "The complexes [RuCp∗(PP)Cl] (Cp∗ = C5Me5; [1], PP = dppm; [4], PP = Xantphos), [RuCp#(PP)Cl] (Cp# = C5Me4(CH2)5OH; [2], PP = dppm; [5], PP = Xantphos) and [RuCp∗(dppm)(CH3CN)][SbF6] [3] were synthesized and evaluated in vitro as anticancer agents. Compounds 1-3 gave nanomolar IC50 values against normoxic A2780 and HT-29 cell lines, and were also tested against hypoxic HT-29 cells, maintaining their high activity. Complex 3 yielded an IC50 value of 0.55 ± 0.03 μM under a 0.1{\%} O2 concentration.",
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Synthesis and anticancer activity evaluation of η5-C5(CH3)4R ruthenium complexes bearing chelating diphosphine ligands. / Rodríguez-Bárzano, A.; Lord, R. M.; Basri, A. M.; Phillips, R. M.; Blacker, A. J.; McGowan, P. C.

In: Dalton Transactions, Vol. 44, No. 7, 05.01.2015, p. 3265-3270.

Research output: Contribution to journalArticle

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AU - Rodríguez-Bárzano, A.

AU - Lord, R. M.

AU - Basri, A. M.

AU - Phillips, R. M.

AU - Blacker, A. J.

AU - McGowan, P. C.

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AB - The complexes [RuCp∗(PP)Cl] (Cp∗ = C5Me5; [1], PP = dppm; [4], PP = Xantphos), [RuCp#(PP)Cl] (Cp# = C5Me4(CH2)5OH; [2], PP = dppm; [5], PP = Xantphos) and [RuCp∗(dppm)(CH3CN)][SbF6] [3] were synthesized and evaluated in vitro as anticancer agents. Compounds 1-3 gave nanomolar IC50 values against normoxic A2780 and HT-29 cell lines, and were also tested against hypoxic HT-29 cells, maintaining their high activity. Complex 3 yielded an IC50 value of 0.55 ± 0.03 μM under a 0.1% O2 concentration.

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