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

Andrea Rodríguez-Bárzano; Rianne M. Lord; Aida M. Basri; Roger M. Phillips; A. John Blacker; Patrick C. McGowan

doi:10.1039/c4dt02748e

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

Andrea Rodríguez-Bárzano, Rianne M. Lord, Aida M. Basri, Roger M. Phillips, A. John Blacker, Patrick C. McGowan

Research output: Contribution to journal › Article › peer-review

9 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 language	English
Pages (from-to)	3265-3270
Number of pages	6
Journal	Dalton Transactions
Volume	44
DOIs	https://doi.org/10.1039/c4dt02748e
Publication status	Published - 5 Jan 2015

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10.1039/c4dt02748e

https://bradscholars.brad.ac.uk/handle/10454/9498

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

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.",

author = "Andrea Rodr{\'i}guez-B{\'a}rzano and Lord, {Rianne M.} and Basri, {Aida M.} and Phillips, {Roger M.} and Blacker, {A. John} and McGowan, {Patrick C.}",

year = "2015",

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doi = "10.1039/c4dt02748e",

language = "English",

volume = "44",

pages = "3265--3270",

journal = "Dalton Transactions",

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publisher = "Royal Society of Chemistry",

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TY - JOUR

T1 - Synthesis and anticancer activity evaluation of η5-C5(CH3)4R ruthenium complexes bearing chelating diphosphine ligands

AU - Rodríguez-Bárzano, Andrea

AU - Lord, Rianne M.

AU - Basri, Aida M.

AU - Phillips, Roger M.

AU - Blacker, A. John

AU - McGowan, Patrick C.

PY - 2015/1/5

Y1 - 2015/1/5

N2 - 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.

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.

UR - http://www.scopus.com/inward/record.url?eid=2-s2.0-84922675469&partnerID=MN8TOARS

U2 - 10.1039/c4dt02748e

DO - 10.1039/c4dt02748e

M3 - Article

VL - 44

SP - 3265

EP - 3270

JO - Dalton Transactions

JF - Dalton Transactions

SN - 1477-9226

ER -

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

Abstract

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