Inorganics,
Год журнала:
2024,
Номер
12(12), С. 307 - 307
Опубликована: Ноя. 26, 2024
Medicinal
Inorganic
Chemistry
has
provided
oncology
with
metallodrugs
for
cancer
treatment,
including
several
promising
candidate
drugs.
In
particular,
copper(II)
coordination
compounds
phenanthroline
stand
out
as
potential
anticancer
agents.
this
work,
we
used
Differential
Scanning
Calorimetry
and
Electron
Spin
Resonance
to
investigate
the
interaction
of
copper
complexes
[Cu(phen)]2+
[Cu(L-dipeptide)(phenanthroline)
(L-dipeptide:
L-Ala-Gly
L-Ala-Phe))
model
lipid
membranes
(1,2-dipalmitoyl-sn-glycero-3-phosphocholine,
DPPC,
1,2-dipalmitoyl-sn-glycero-3-phospho-(1′-rac-glycerol)
sodium
salt,
DPPG).
Our
results
showed
that
interact
membrane
models,
fluidizing
them.
The
presented
a
different
localization
than
free
ligand
phen.
dipeptide
modulated
complex
in
modifications
induced
physicochemical
properties
vesicles.
A
stronger
DPPG
anionic
was
observed,
which
mimic
negatively
charged
surfaces,
found
on
tumor
cells.
Molecules,
Год журнала:
2024,
Номер
29(5), С. 1066 - 1066
Опубликована: Фев. 29, 2024
Most
diseases
that
affect
human
beings
across
the
world
are
now
treated
with
drugs
of
organic
origin.
However,
some
these
associated
side
effects,
toxicity,
and
resistance
phenomena.
For
treatment
many
illnesses,
development
new
molecules
pharmacological
potential
is
an
urgent
matter.
The
biological
activities
metal
complexes
have
been
reported
to
antitumor,
antimicrobial,
anti-inflammatory,
anti-infective
antiparasitic
amongst
others.
Metal
effective
because
they
possess
unique
properties.
example,
complex
entity
possesses
activity,
then
formation
coordination
bonds
between
ions
ligands
controlled,
provide
it
extraordinary
mechanisms
action
characteristics
such
as
d-orbitals,
oxidation
states,
specific
orientations;
also
exhibit
good
stability
physicochemical
properties
water
solubility.
Platinum
a
transition
widely
used
in
design
antineoplastic
activities;
however,
platinum
effects
which
made
necessary
search
for,
design,
novel
based
on
other
metals.
Copper
biometal
found
living
systems;
demonstrated
antitumoral,
antimicrobial
anti-inflammatory
In
this
review,
we
consider
open
horizons
Cu(II)-
Pt(II)-based
complexes,
trends
their
synthesis,
targets
action.
International Journal of Molecular Sciences,
Год журнала:
2024,
Номер
25(10), С. 5283 - 5283
Опубликована: Май 13, 2024
The
interactions
with
calf
thymus
DNA
(CT-DNA)
of
three
Schiff
bases
formed
by
the
condensation
hesperetin
benzohydrazide
(HHSB
or
L1H3),
isoniazid
(HIN
L2H3),
thiosemicarbazide
(HTSC
L3H3)
and
their
CuII
complexes
(CuHHSB,
CuHIN,
CuHTSC
general
formula
[CuLnH2(AcO)])
were
evaluated
in
aqueous
solution
both
experimentally
theoretically.
UV–Vis
studies
indicate
that
ligands
exhibit
hypochromism,
which
suggests
helical
ordering
helix.
intrinsic
binding
constants
(Kb)
Cu
compounds
CT-DNA,
range
(2.3–9.2)
×
106,
from
to
CuHHSB,
higher
than
other
copper-based
potential
drugs,
suggesting
π–π
stacking
interaction
due
presence
aromatic
rings
favors
binding.
Thiazole
orange
(TO)
assays
confirmed
displace
TO
site,
quenching
fluorescence
emission.
DFT
calculations
allow
for
an
assessment
equilibrium
between
[Cu(LnH2)(AcO)]
[Cu(LnH2)(H2O)]+,
tautomer
binds
CuII,
amido
(am)
not
imido
(im),
coordination
mode
HTSC
(O−,
N,
S),
instead
NH2).
docking
intercalative
is
preferred
over
minor
groove
CT-DNA
order
[Cu(L1H2am)(AcO)]
>
[Cu(L2H2am)(AcO)]
≈
L1H3
[Cu(L3H2am)(AcO)],
line
experimental
Kb
constants,
obtained
spectroscopy.
Moreover,
dockings
predict
strength
larger
[Cu(L1H2am)(H2O)]+.
Overall,
results
suggest
when
different
enantiomers,
tautomers,
donor
sets
are
possible
a
metal
complex,
computational
approach
should
be
recommended
type
and,
general,
macromolecules.
Molecules,
Год журнала:
2025,
Номер
30(2), С. 313 - 313
Опубликована: Янв. 15, 2025
The
interaction
of
sodium
phytate
hydrate
C6H18O24P6·xNa·yH2O
(phytNa)
with
Cu(OAc)2·H2O
and
1,10-phenanthroline
(phen)
led
to
the
anionic
tetranuclear
complex
[Cu4(H2O)4(phen)4(phyt)]·2Na+·2NH4+·32H2O
(1),
structure
latter
was
determined
by
X-ray
diffraction
analysis.
1
is
completely
deprotonated;
six
phosphate−
fragments
(with
atoms
P1–P6)
are
characterized
different
spatial
arrangements
relative
cyclohexane
ring
(1a5e
conformation),
which
determines
two
types
coordination
complexing
agents—P1
P3,
P4,
P6
have
monodentate,
while
P2
P5
bidentately
bound
Cu2+
cations.
molecular
anion
stabilized
a
set
strong
intramolecular
hydrogen
bonds
involving
coordinated
water
molecules.
Aromatic
systems
phen
ligands
chelating
copper
ions
participate
in
intermolecular
π-π
interactions,
further
contributing
their
association.
At
supramolecular
level,
endless
stacks
formed,
voids
ammonium
cations
molecules
present.
stability
presence
human
serum
albumin
(HSA)
investigated
using
Electron
Paramagnetic
Resonance
(EPR)
spectroscopy.
Continuous
wave
(CW)
EPR
spectra
water/glycerol
frozen
solution
clearly
indicate
an
exchange-coupled
Cu(II)-Cu(II)
dimeric
unit,
as
well
Cu(II)
monomer-like
signal
arising
from
spins
sufficiently
distant
each
other,
comparable
contributions
signals.
In
at
1:1
ratio
(1
albumin),
spectrum
changes
significantly,
primarily
due
reduced
contribution
S
=
fraction
showing
dipole–dipole
splitting.
biological
activity
vitro
against
non-pathogenic
(model
for
Mycobacterium
tuberculosis)
strain
Mycolicibacterium
smegmatis
first-line
drug
tuberculosis
treatment,
rifampicin.
Bioconjugate Chemistry,
Год журнала:
2025,
Номер
unknown
Опубликована: Март 10, 2025
Cu(II)
coordination
complexes
are
emerging
as
promising
anticancer
agents
due
to
their
ability
induce
oxidative
stress
through
reactive
oxygen
species
(ROS)
generation.
In
this
study,
we
synthesized
and
characterized
two
novel
metallopeptide
systems,
1/Cu(II)
2/Cu(II),
derived
from
the
oligocationic
bipyridyl
cyclopeptides
1
2,
designed
enhance
transport
of
into
cells
increase
ROS
levels.
Spectroscopic
electrochemical
analyses
confirmed
formation
stable
in
aqueous
media.
Inductively
coupled
plasma
mass
spectrometry
(ICP-MS)
studies
demonstrated
that
both
metallopeptides
significantly
intracellular
accumulation
NCI/ADR-RES
cancer
cells,
highlighting
role
efficient
transporters.
Additionally,
generation
assays
revealed
induces
a
substantial
levels,
supporting
hypothesis
stress-induced
cytotoxicity.
Cell-viability
further
2/Cu(II)
exhibit
strong
activity
number
cell
lines,
with
IC50
values
lower
than
those
free
cyclopeptide
counterparts
or
alone,
showing
an
order
higher
cisplatin.
Finally,
molecular
modeling
provided
insights
structural
stability
environment
within
complexes.
These
findings
suggest
these
cyclometallopeptide
systems
hold
potential
metal-based
therapeutic
agents,
leveraging
key
strategies
for
treatment.
International Journal of Molecular Sciences,
Год журнала:
2024,
Номер
25(4), С. 2038 - 2038
Опубликована: Фев. 7, 2024
The
3d
transition
metal
(Mn(II),
Fe(II),
Co(II),
Ni(II),
Cu(II)
and
Zn(II))
complexes,
supported
by
anions
of
sterically
demanding
β-diketones,
1,3-dimesitylpropane-1,3-dione
(HLMes)
1,3-bis(3,5-bis(trifluoromethyl)phenyl)-3-hydroxyprop-2-en-1-one
(HLCF3),
were
synthesized
evaluated
for
their
antitumor
activity.
To
assess
the
biological
effects
substituents
on
phenyl
moieties,
we
also
investigated
analogous
metal(II)
complexes
anion
less
bulky
1,3-diphenylpropane-1,3-dione
(HLPh)
ligand.
compounds
[Cu(LCF3)2],
[Cu(LMes)2]
([Zn(LMes)2])
characterized
X-ray
crystallography.
[Cu(LCF3)2]
crystallizes
with
an
apical
molecule
solvent
(THF)
features
a
rare
square
pyramidal
geometry
at
center.
copper(II)
zinc(II)
diketonate
ligands,
derived
from
deprotonated
(HLMes),
adopt
planar
or
tetrahedral
metal,
respectively.
We
properties
newly
against
series
human
tumor
cell
lines
different
solid
tumors.
Except
iron
derivatives,
cellular
studies
revealed
noteworthy
properties,
even
towards
cancer
cells
endowed
poor
sensitivity
to
reference
drug
cisplatin.