TY - JOUR
T1 - Bis(bipyridine)ruthenium(II) ferrocenyl β-diketonate complexes
T2 - exhibiting nanomolar potency against human cancer cell lines
AU - Allison, Matthew
AU - Caramés-Méndez, Pablo
AU - Pask, Christopher M.
AU - Phillips, Roger
AU - Lord, Rianne M.
AU - McGowan, Patrick C.
N1 - Funding Information:
We would like to thank the Community for Open Antimicrobial Drug Discovery (CO-ADD) at The University of Queensland for the screening of our complexes against bacterial and fungal strains. We also thank Ms. Tanya Marinko-Covell (University of Leeds) and Mr. Stephen Boyer (London Metropolitan University) for elemental analysis services. We would like to acknowledge the University of Leeds (MA) and the Henry Ellison Scholarship (P. C.-M.) for PhD studentships, the University of Huddersfield and the Institute of Cancer Therapeutics (University of Bradford) both for cell culture facilities and the University of Bradford's research development fund which was awarded to RML.
Publisher Copyright:
© 2020 Wiley-VCH GmbH
Copyright:
Copyright 2021 Elsevier B.V., All rights reserved.
PY - 2021/2/19
Y1 - 2021/2/19
N2 - The synthesis and characterization of new bis(bipyridine)ruthenium(II) ferrocenyl β-diketonate complexes, [(bpy)
2Ru(Fc-acac)][PF
6] (bpy=2,2′-bipyridine; Fc-acac=functionalized ferrocenyl β-diketonate ligand) are reported. Alongside clinical platinum drugs, these bimetallic ruthenium-iron complexes have been screened for their cytotoxicity against MIA PaCa-2 (human pancreatic carcinoma), HCT116 p53
+/+ (human colon carcinoma, p53-wild type) and ARPE-19 (human retinal pigment epithelial) cell lines. With the exception of one complex, the library exhibit nanomolar potency against cancerous cell lines, and their relative potencies are up to 40x, 400x and 72x more cytotoxic than cisplatin, carboplatin and oxaliplatin, respectively. Under hypoxic conditions, the complexes remain cytotoxic (sub-micromolar range), highlighting their potential in targeting hypoxic tumor regions. The Comet assay was used to determine their ability to damage DNA, and results show dose dependent damage which correlates well with the cytotoxicity results. Their potential to treat bacterial and fungal strains has been determined, and highlight complexes have selective growth inhibition of up to 87–100 % against Staphylococcus aureus and Candida albicans.
AB - The synthesis and characterization of new bis(bipyridine)ruthenium(II) ferrocenyl β-diketonate complexes, [(bpy)
2Ru(Fc-acac)][PF
6] (bpy=2,2′-bipyridine; Fc-acac=functionalized ferrocenyl β-diketonate ligand) are reported. Alongside clinical platinum drugs, these bimetallic ruthenium-iron complexes have been screened for their cytotoxicity against MIA PaCa-2 (human pancreatic carcinoma), HCT116 p53
+/+ (human colon carcinoma, p53-wild type) and ARPE-19 (human retinal pigment epithelial) cell lines. With the exception of one complex, the library exhibit nanomolar potency against cancerous cell lines, and their relative potencies are up to 40x, 400x and 72x more cytotoxic than cisplatin, carboplatin and oxaliplatin, respectively. Under hypoxic conditions, the complexes remain cytotoxic (sub-micromolar range), highlighting their potential in targeting hypoxic tumor regions. The Comet assay was used to determine their ability to damage DNA, and results show dose dependent damage which correlates well with the cytotoxicity results. Their potential to treat bacterial and fungal strains has been determined, and highlight complexes have selective growth inhibition of up to 87–100 % against Staphylococcus aureus and Candida albicans.
KW - Bioinorganic
KW - Cancer
KW - Hetero-bimetallic
KW - Iron
KW - Ruthenium
KW - bioinorganic
KW - ruthenium
KW - hetero-bimetallic
KW - iron
KW - cancer
UR - http://www.scopus.com/inward/record.url?scp=85099484950&partnerID=8YFLogxK
U2 - 10.1002/chem.202004024
DO - 10.1002/chem.202004024
M3 - Article
VL - 27
SP - 3737
EP - 3744
JO - Chemistry - A European Journal
JF - Chemistry - A European Journal
SN - 0947-6539
IS - 11
ER -
