International Journal of Molecular Sciences,
Год журнала:
2023,
Номер
25(1), С. 8 - 8
Опубликована: Дек. 19, 2023
Four
copper(II)
complexes,
C1–4,
derived
from
1-(isoquinolin-3-yl)heteroalkyl-2-one
ligands
L1–4
were
synthesized
and
characterized
using
an
elemental
analysis,
IR
spectroscopic
data
as
well
single
crystal
X-ray
diffraction
for
complex
C1.
The
stability
of
complexes
C1–4
under
conditions
mimicking
the
physiological
environment
was
estimated
UV-Vis
spectrophotometry.
antiproliferative
activity
both
compounds
evaluated
MTT
assay
on
four
human
cancer
cell
lines,
A375
(melanoma),
HepG2
(hepatoma),
LS-180
(colon
cancer)
T98G
(glioblastoma),
a
non-cancerous
line,
CCD-1059Sk
(human
normal
skin
fibroblasts).
Complexes
showed
greater
potency
against
HepG2,
LS180
lines
than
etoposide
(IC50
=
5.04–14.89
μg/mL
vs.
IC50
43.21–>100
μg/mL),
while
free
remained
inactive
in
all
lines.
prominent
compound
C2
appeared
to
be
more
selective
towards
cells
compared
with
C1,
C3
C4.
treatment
resulted
sub-G1
G2/M
cycle
arrest,
respectively,
which
accompanied
by
DNA
degradation.
Moreover,
non-cytotoxic
doses
synergistically
enhanced
cytotoxic
effects
chemotherapeutic
drugs,
including
etoposide,
5-fluorouracil
temozolomide,
cells.
antimicrobial
activities
L2–4
their
C2–4
different
types
Gram-positive
bacteria,
Gram-negative
bacteria
yeast
species.
No
correlation
found
between
results
experiments.
antioxidant
determined
DPPH
ABTS
radical
scavenging
methods.
Antiradical
tests
revealed
that
among
investigated
compounds,
C4
possessed
strongest
properties.
Finally,
ADME
technique
used
determine
physicochemical
drug-likeness
properties
obtained
complexes.
Chemistry - A European Journal,
Год журнала:
2024,
Номер
30(10)
Опубликована: Янв. 3, 2024
Abstract
Platinum
complexes
are
potential
antitumor
drugs
in
chemotherapy.
Their
impact
on
tumor
treatment
could
be
greatly
strengthened
by
combining
with
immunotherapy.
Increasing
evidences
indicate
that
the
activity
of
platinum
is
not
limited
to
chemical
killing
effects,
but
also
extends
immunomodulatory
actions.
This
review
introduced
general
concept
chemoimmunotherapy
and
summarized
progress
as
chemoimmunotherapeutic
agents
recent
years.
developed
into
inducers
immunogenic
cell
death,
blockers
immune
checkpoint,
regulators
signaling
pathway,
modulators
microenvironment,
etc.
The
synergy
between
chemotherapeutic
effects
reinforces
complexes,
helps
them
circumvent
drug
resistance
systemic
toxicity.
exploration
for
may
create
new
opportunities
revive
discovery
metal
anticancer
drugs.
Journal of Medicinal Chemistry,
Год журнала:
2024,
Номер
67(3), С. 2031 - 2048
Опубликована: Янв. 17, 2024
Metastasis
is
the
major
obstacle
to
survival
of
cancer
patients.
Herein,
a
series
new
desloratadine
platinum(IV)
conjugates
with
promising
antiproliferative
and
antimetastatic
activities
were
developed
evaluated.
The
candidate
complex
caused
significant
DNA
damage
stimulated
mitochondrial
apoptosis
through
Bcl-2/Bax/caspase3
pathway.
Then,
it
suppressed
epithelial–mesenchymal
transition
(EMT)
process
in
tumors
effectively
NMT-1/HPCAL1
β-catenin
signaling.
Subsequently,
angiogenesis
was
inhibited
downregulation
key
proteins
HIF-1α,
VEGFA,
MMP-9,
CD34.
Moreover,
antitumor
immunity
aroused
by
synergism
EMT
reversion
decrease
histamine
level;
then,
macrophage
polarization
from
M2-
M1-type
increase
CD4+
CD8+
T
cells
triggered
simultaneously
tumors.
ACS Omega,
Год журнала:
2024,
Номер
9(2), С. 2650 - 2656
Опубликована: Янв. 3, 2024
The
stimulator
of
interferon
genes
(STING)-activated
innate
immune
pathway
is
strong
and
durable
for
tumor
immunotherapy.
MSA-2
an
available
non-nucleotide
human
STING
agonist
that
promotes
the
immunotherapy
activation.
However,
strategies
remolding
improving
effects
are
value
clinical
applications.
Here,
we
synthesized
platinum
salt-modified
(MSA-2-Pt)
due
to
salt
being
a
classic
chemotherapeutic
drug.
We
found
MSA-2-Pt
could
achieve
double-effect
antitumor
immunotherapy,
including
inducing
cell
death
by
activating
MSA-2.
In
colon
carcinoma
MC38
model
(sensitive
checkpoint
tumor)
melanoma
B16F10
(poorly
immunogenic
highly
aggressive
tumor),
had
good
effect,
which
was
little
better
than
with
intratumor
injections.
results
present
promising
strategy
activation
in
broadening
platinum-based
drugs.
Langmuir,
Год журнала:
2024,
Номер
40(23), С. 12226 - 12238
Опубликована: Май 30, 2024
We
have
red-shifted
the
light
absorbance
property
of
a
Re(I)-tricarbonyl
complex
via
distant
conjugation
ferrocene
moiety
and
developed
novel
ReFctp,
[Re(Fctp)(CO)3Cl],
where
Fctp
=
4′-ferrocenyl-2,2′:6′,2″-terpyridine.
ReFctp
showed
green
to
red
absorption
ability
blue
emission,
indicating
its
potential
for
photodynamic
therapy
(PDT)
application.
The
introduced
ferrocene-based
transitions,
which
lie
at
higher
wavelength
within
PDT
therapeutic
window.
time-dependent
density
functional
theory
excited
state
calculations
revealed
an
efficient
intersystem
crossing
is
helpful
PDT.
elicited
both
type
I
II
pathways
reactive
oxygen
species
(ROS)
generation
facilitated
NADH
(1,4-dihydro-nicotinamide
adenine
dinucleotide)
oxidation
upon
exposure
visible
light.
Importantly,
effective
penetration
through
layers
clinically
relevant
3D
multicellular
tumor
spheroids
localized
primarily
in
mitochondria
(Pearson's
correlation
coefficient,
PCC
0.65)
A549
cancer
cells.
produced
more
than
20
times
phototoxicity
(IC50
∼1.5
μM)
by
inducing
ROS
altering
mitochondrial
membrane
cells
nonferrocene
analogue
Retp,
[Re(CO)3(tp)Cl],
tp
2,2′:6′,2″-terpyridine.
induced
apoptotic
mode
cell
death
with
notable
photocytotoxicity
index
(PI,
PI
IC50dark/IC50light)
selectivity
(SI,
SI
normal
cell's
IC50dark/cancer
IC50light)
range
25–33.
Dalton Transactions,
Год журнала:
2025,
Номер
unknown
Опубликована: Янв. 1, 2025
Photoactive
complexes
of
bioessential
3d
metals,
activable
within
the
phototherapeutic
window
(650-900
nm),
have
gained
widespread
interest
due
to
their
therapeutic
potential.
Herein,
we
report
synthesis,
characterization,
and
light-enhanced
anticancer
antibacterial
properties
four
new
dinuclear
Co(II)
complexes:
[Co(phen)(cat)]2
(Co-1),
[Co(dppz)(cat)]2
(Co-2),
[Co(phen)(esc)]2
(Co-3),
[Co(dppz)(esc)]2
(Co-4).
In
these
complexes,
phen
(1,10-phenanthroline)
dppz
(dipyrido[3,2-a:2',3'-c]phenazine)
act
as
neutral
N,N-donor
ligands,
while
cat2-
esc2-
serve
O,O-donor
catecholate
ligands
derived
from
catechol
(1,2-dihydroxybenzene)
esculetin
(6,7-dihydroxy
coumarin).
Their
high-spin
paramagnetic
nature
dimeric
identity
in
solution
were
confirmed
by
magnetic
susceptibility,
UV-visible,
emission,
mass
spectral
data.
Co-1-Co-4
exhibited
an
absorption
band
600-850
nm
range,
originating
a
charge
transfer
transition.
The
electrically
demonstrated
sufficient
stability
both
dark
under
irradiated
conditions.
Co-2
Co-4
notable
toxicity
towards
A549
lung
carcinoma
cells,
with
potency
increasing
significantly
brief
(5
min)
exposure
660
(red)
808
(NIR)
laser
light
(IC50
∼
8.9
14.9
μM).
Notably,
normal
NIH-3T3
fibroblast
cells
was
minimal.
Cellular
assays
highlighted
that
induced
cell
death
followed
apoptotic
pathway,
primarily
mitochondrial
damage.
also
significant
against
Gram-(+)
S.
aureus
Gram-(-)
P.
aeruginosa,
effectiveness
enhanced
upon
irradiation
(MIC
15-142
increase
efficacies
attributed
generation
cytotoxic
singlet
oxygen
(1O2)
species
red/NIR
exposure.
NIR
produced
more
pronounced
effects
compared
nm.
This
study
is
first
on
cobalt
exhibiting
red
light-triggered
enhancement
activities,
illuminating
path
for
development
long-wavelength
absorbing
efficacy.
Chemistry - A European Journal,
Год журнала:
2024,
Номер
30(32)
Опубликована: Апрель 4, 2024
Abstract
Cancer
is
one
of
the
deadliest
diseases
worldwide.
Chemotherapy
remains
most
dominant
forms
for
anticancer
treatment.
Despite
their
clinical
success,
used
chemotherapeutic
agents
are
associated
with
severe
side
effect
and
pharmacological
limitations.
To
overcome
these
drawbacks
there
a
need
development
new
types
agents.
Herein,
chemical
synthesis
biological
evaluation
dinuclear
rhenium(I)
complexes
as
potential
drug
candidates
proposed.
The
metal
were
found
to
be
internalized
by
an
energy
dependent
endocytosis
pathway,
primary
accumulating
in
mitochondria.
demonstrated
induce
cell
death
against
variety
cancer
cells
micromolar
range
through
apoptosis.
lead
compound
showed
eradicate
pancreatic
carcinoma
multicellular
tumor
spheroid
at
concentrations.
