10.1021/jm4007615.s002
Nicholas Lease
Nicholas
Lease
Vadim Vasilevski
Vadim
Vasilevski
Monica Carreira
Monica
Carreira
Andreia de Almeida
Andreia de
Almeida
Mercedes Sanaú
Mercedes
Sanaú
Pipsa Hirva
Pipsa
Hirva
Angela Casini
Angela
Casini
María Contel
María
Contel
Potential
Anticancer Heterometallic Fe–Au and
Fe–Pd Agents: Initial Mechanistic Insights
American Chemical Society
2013
cisplatin
PARP
kidney cell line
2780R
2780S
cytotoxic trimetallic derivatives M 2Fe
MCF 7 cell lines
PdCl
breast cancer cells
cancer cells
DNA
HEK
complex
Initial Mechanistic InsightsA series
AuCl
2013-07-25 00:00:00
Dataset
https://acs.figshare.com/articles/dataset/Potential_Anticancer_Heterometallic_Fe_Au_and_Fe_Pd_Agents_Initial_Mechanistic_Insights/2392906
A series of gold(III) and palladium(II)
heterometallic complexes
with new iminophosphorane ligands derived from ferrocenylphosphanes
[{Cp-P(Ph<sub>2</sub>)N-Ph}<sub>2</sub>Fe] (<b>1</b>), [{Cp-P(Ph<sub>2</sub>)N-CH<sub>2</sub>-2-NC<sub>5</sub>H<sub>4</sub>}<sub>2</sub>Fe] (<b>2</b>), and [{Cp-P(Ph<sub>2</sub>)N-CH<sub>2</sub>-2-NC<sub>5</sub>H<sub>4</sub>}Fe(Cp)]
(<b>3</b>) have been synthesized and structurally characterized.
Ligands <b>2</b> and <b>3</b> afford stable coordination
complexes [AuCl<sub>2</sub>(<b>3</b>)]ClO<sub>4</sub>, [{AuCl<sub>2</sub>}<sub>2</sub>(<b>2</b>)](ClO<sub>4</sub>)<sub>2</sub>, [PdCl<sub>2</sub>(<b>3</b>)], and [{PdCl<sub>2</sub>}<sub>2</sub>(<b>2</b>)]. The complexes have been evaluated for their
antiproliferative properties in human ovarian cancer cells sensitive
and resistant to cisplatin (A2780S/R), in human breast cancer cells
(MCF7) and in a nontumorigenic human embryonic kidney cell line (HEK-293T).
The highly cytotoxic trimetallic derivatives M<sub>2</sub>Fe (M =
Au, Pd) are more cytotoxic to cancer cells than their corresponding
monometallic fragments. Moreover, these complexes were significantly
more cytotoxic than cisplatin in the resistant A2780R and the MCF7
cell lines. Studies of the interactions of the trimetallic compounds
with DNA and the zinc-finger protein PARP-1 indicate that they exert
anticancer effects in vitro based on different mechanisms of actions
with respect to cisplatin.