Optimizing Therapeutics for Intratumoral Cancer Treatments: Antiproliferative Vanadium Complexes in Glioblastoma
International Journal of Molecular Sciences,
Год журнала:
2025,
Номер
26(3), С. 994 - 994
Опубликована: Янв. 24, 2025
Glioblastoma,
an
aggressive
cancer,
is
difficult
to
treat
due
its
location,
late
detection,
drug
resistance,
and
poor
absorption
of
chemotherapeutics.
Intratumoral
administration
offers
a
promising
potential
treatment
alternative
with
localized
delivery
minimal
systemic
toxicity.
Vanadium(V)
coordination
complexes,
incorporating
Schiff
base
catecholate
ligands,
have
shown
effects
as
antiproliferative
agents
tunable
efficacy
reactivity,
stability,
steric
bulk,
hydrophobicity,
uptake,
toxicity
optimized
for
the
intratumoral
vehicle.
A
new
series
oxovanadium(V)
base–catecholate
complexes
were
synthesized
characterized
using
nuclear
magnetic
resonance
(NMR),
UV-Vis,
infrared
spectroscopy
mass
spectrometry.
Stability
under
physiological
conditions
was
assessed
via
UV-Vis
spectroscopy,
activity
evaluated
in
T98G
glioblastoma
SVG
p12
normal
glial
cells
viability
assays.
The
newly
[VO(3-tBuHSHED)(TIPCAT)]
complex
more
stable
(t1/2
~
4.5
h)
had
strong
(IC50
1.5
µM),
comparing
favorably
current
lead
compound,
[VO(HSHED)(DTB)].
structural
modifications
enhanced
bulk
through
substitution
iso-propyl
tert-butyl
groups.
improved
properties
attributed
hindrance
associated
catecholato
well
formation
non-toxic
byproducts
upon
degradation.
emerges
candidate
therapy
by
demonstrating
stability
greater
selectivity,
which
highlights
role
strategic
ligand
design
developing
therapies
resistant
cancers.
In
reporting
class
compounds
effective
against
cells,
we
describe
generally
desirable
that
drugs
being
developed
should
have.
Язык: Английский
Reactivity in cell culture medium and in vitro anticancer activity of 3,5-di-tert-butylcatechol: link to metal-catechol interactions
Frontiers in Chemical Biology,
Год журнала:
2025,
Номер
4
Опубликована: Фев. 3, 2025
Introduction
Catechol
moieties
are
common
in
natural
bioactive
molecules,
and
their
ability
to
bind
metal
ions
is
widely
explored
both
naturally
with
siderophores
the
development
of
metal-based
drugs.
The
reactivities
biology
activities
a
sterically
hindered
model
catechol
compound,
3,5-di-
tert
-butylcatechol
(dtbH
2
)
its
oxidation
product
-butyl-
o
-quinone
(dtbQ),
were
studied
cell
culture
medium
understand
better
medicinal
roles
this
class
molecules.
Methods
Anti-proliferative
dtbH
dtbQ
fresh
aged
solutions
molecules
two
human
cancer
lines,
T98G
(glioblastoma)
A549
(lung
carcinoma).
Electrospray
mass
spectrometry
UV/Vis
spectroscopy
used
study
buffer
medium,
presence
absence
glutathione
imidazole.
Results
Discussion
showed
high
anti-proliferative
activity
(IC
50
<
10
μM
72
h
assays)
lines
added
ions.
was
observed
when
freshly
while
pre-incubation
for
24
reduced
5-10-fold.
This
deactivation
avoided
biological
reductant,
(GSH),
at
physiologically
relevant
intracellular
concentration
(5.0
mM).
These
results
explained
by
speciation
studies
(UV/Vis
spectrometry)
aqueous
buffers,
or
organic
solvents
GSH.
that
redox
equilibrium
established
between
dtbQ,
latter
rapidly
coupling
GSH
an
oxidative
manner.
resultant
adduct
likely
be
responsible
toxicity
GSH-rich
cells
via
oxygen-dependent
radical
chain
reactions.
Deactivation
due
reactions
nucleophiles,
such
as
amino
acids,
followed
formation
polymeric
species.
reported
V(V)-catecholato
complexes
can
combination
efficient
cellular
uptake
rapid
decomposition
thiol-rich
environment
active
V(V)
/dtbQ
adducts
thiols
(mainly
GSH).
Slower
thiol-poor
extracellular
environments.
data
show
crucial
not
only
but
also
ligands
dissociates.
Язык: Английский
Recent advances of Schiff base metal complexes as potential anticancer agents
Coordination Chemistry Reviews,
Год журнала:
2024,
Номер
525, С. 216327 - 216327
Опубликована: Ноя. 20, 2024
Язык: Английский
Exploring the Potential of N‐Benzylidenebenzohydrazide Derivatives as Antidiabetic and Antioxidant Agents: Design, Synthesis, Spectroscopic, Crystal Structure, DFT and Molecular Docking Study
ChemistrySelect,
Год журнала:
2024,
Номер
9(35)
Опубликована: Сен. 12, 2024
Abstract
Hydrazone‐type
Schiff
bases
have
been
widely
explored
owing
to
their
therapeutic
properties.
These
compounds
are
known
antibacterial,
antifungal,
anticancer,
and
antioxidant
properties,
among
others.
In
the
present
study,
six
hydrazone‐based
(
BB1
–
BB6
)
were
synthesized
by
reaction
between
derivatives
of
benzaldehyde
benzo
hydrazide
in
methanolic
medium
presence
catalytic
amount
formic
acid.
The
characterized
using
various
spectroscopic
techniques
such
as
NMR
1
H,
13
C,
COSY,
DEPT,
HSQC,
HMBC,
NOESY),
FTIR,
UV‐Vis,
elemental
(CHN)
analysis,
high‐resolution
mass
spectroscopy.
addition,
single
crystal
structures
BB2
,
BB4
obtained.
vitro
antidiabetic
potential
was
evaluated
on
glucosidase,
amylase,
NO,
FRAP,
DPPH
assays,
respectively.
all
showed
higher
activity
than
To
further
explore
chemical
reactivity
properties
mechanism
action
against
tested
DFT
molecular
docking
study
performed,
results
obtained
reinforce
experimental
data.
Язык: Английский