Dalton Transactions,
Год журнала:
2022,
Номер
51(31), С. 11713 - 11729
Опубликована: Янв. 1, 2022
To
validate
the
effect
of
metal
ions
in
analogous
ligand
scaffolds
on
DNA
binding
and
cytotoxic
response,
we
have
synthesized
a
series
water-soluble
ionic
N-phthaloylglycinate
conjugated
bis(diaminocyclohexane)M2+
complexes
where
M
=
Ni(II),
Cu(II)
Zn(II)
(1-3).
The
structural
characterization
(1-3)
was
achieved
by
spectroscopic
{FT-IR,
EPR,
UV-vis
absorption
data,
1H
NMR,
ESI-MS
elemental
analysis}
single
crystal
X-ray
diffraction
studies,
which
revealed
different
topologies
for
late
3d-transition
metals.
Ni(II)
exhibited
an
octahedral
geometry
with
coordinated
labile
water
molecules
P1̄
space
group
while
complex
square
planar
P21/c
lattice.
In
vitro
DNA-complexation
studies
were
performed
employing
various
complementary
biophysical
methods
to
quantify
intrinsic
constant
Kb
Ksv
values
envisage
modes
affinity
at
therapeutic
targets.
corroborative
results
these
experiments
substantial
geometric
electronic
following
inferences
observed,
(i)
high
values,
(ii)
remarkable
cleavage
efficiency
via
oxidative
pathway,
(iii)
condensation
behavior
(iv)
good
response
HepG2
PTEN-caP8
cancer
cell
lines,
copper(II)
2
outperforming
other
two
as
most
promising
anticancer
drug
candidate.
Copper(II)
been
proven
literature
be
entities,
displaying
inhibition
uncontrolled-cell
growth
multiple
pathways
viz.,
anti-angiogenesis,
inducing
apoptosis
reactive
oxygen
species
mediated
death
phenomena.
Nickel(II)
zinc(II)
1
3
also
demonstrated
chemotherapeutic
potential
bioactive
1,2-diaminocyclohexane
fragment
plays
instrumental
role
activity.
Phytotherapy Research,
Год журнала:
2024,
Номер
38(8), С. 3877 - 3898
Опубликована: Май 20, 2024
Abstract
Resveratrol
is
a
widely
recognized
polyphenolic
phytochemical
found
in
various
plants
and
their
fruits,
such
as
peanuts,
grapes,
berry
fruits.
It
renowned
for
its
several
health
advantages.
The
well
known
anticancer
properties,
substantial
amount
of
clinical
evidence
has
also
established
promise
chemotherapeutic
agent.
This
study
focuses
on
assessing
the
properties
resveratrol
gaining
insight
into
underlying
molecular
mechanisms.
evaluates
biopharmaceutical,
toxicological
characteristics,
utilization
to
determine
suitability
further
development
reliable
Therefore,
information
about
preclinical
studies
was
collected
from
different
electronic
databases
up‐to‐date
(2018–2023).
Findings
this
revealed
that
potent
therapeutic
benefits
against
cancers
involving
mechanisms,
induction
oxidative
stress,
cytotoxicity,
inhibition
cell
migration
invasion,
autophagy,
arresting
S
phase
cycle,
apoptotic,
anti‐angiogenic,
antiproliferative
effects
by
regulating
pathways
including
PI3K/AKT,
p38/MAPK/ERK,
NGFR‐AMPK‐mTOR,
so
on.
However,
compound
poor
oral
bioavailability
due
reduced
absorption;
limitation
overcome
applying
nanotechnology
(nanoformulation
resveratrol).
Clinical
application
showed
types
cancer
with
no
serious
adverse
effects.
We
suggest
additional
extensive
check
efficacy,
safety,
long‐term
hazards.
could
involve
larger
number
samples
establish
drug
treatment
cancer.
Molecules,
Год журнала:
2023,
Номер
28(15), С. 5678 - 5678
Опубликована: Июль 27, 2023
Napabucasin
(also
known
as
BBI608)
is
a
natural
naphthoquinone
originally
identified
cancer
cell
stemness
inhibitor.
Accumulated
in
vitro
and
vivo
evidence
demonstrated
that
napabucasin
showed
significant
anticancer
effects
various
types
of
cancers.
inhibits
proliferation,
induces
apoptosis
cycle
arrest,
suppresses
metastasis
relapse.
Such
activities
mainly
rely
on
the
inhibition
by
targeting
signal
transducer
activator
transcription
3
(STAT3)
its
related
gene
inhibition.
However,
several
novel
molecular
targets
for
napabucasin,
such
NAD(P)H:quinone
oxidoreductase
1
(NQO1)
thioredoxin
reductase
(TrxR1),
have
been
reported.
represents
promising
lead
multiple
In
this
mini
review,
potential
mechanism
will
be
briefly
highlighted.
Journal of Medicinal Chemistry,
Год журнала:
2024,
Номер
67(5), С. 4170 - 4193
Опубликована: Март 4, 2024
We
report
here
the
first
dual
inhibitors
of
brain
carbonic
anhydrases
(CAs)
and
monoamine
oxidase-B
(MAO-B)
for
management
Alzheimer's
disease.
Classical
CA
(CAIs)
such
as
methazolamide
prevent
amyloid-β-peptide
(Aβ)-induced
overproduction
reactive
oxygen
species
(ROS)
mitochondrial
dysfunction.
MAO-B
is
also
implicated
in
ROS
production,
cholinergic
system
disruption,
amyloid
plaque
formation.
In
this
work,
we
combined
a
reversible
inhibitor
coumarin
chromone
type
with
benzenesulfonamide
fragments
highly
effective
CAIs.
A
hit-to-lead
optimization
led
to
significant
set
derivatives
showing
potent
low
nanomolar
inhibition
target
CAs
(KIs
range
0.1–90.0
nM)
(IC50
6.7–32.6
nM).
Computational
studies
were
conducted
elucidate
structure–activity
relationship
predict
ADMET
properties.
The
most
multitarget
compounds
totally
prevented
Aβ-related
toxicity,
reverted
formation,
restored
functionality
an
SH-SY5Y
cell
model
surpassing
efficacy
single-target
drugs.
Advanced Materials,
Год журнала:
2024,
Номер
unknown
Опубликована: Июль 23, 2024
Abstract
Despite
the
promise
of
activatable
chemotherapy,
development
a
spatiotemporally
controllable
strategy
for
prodrug
activation
in
deep
tissues
remains
challenging.
Herein,
proof‐of‐concept
is
proposed
gold
nanocluster‐based
that
utilizes
X‐ray
irradiation
to
trigger
liberation
platinum
(Pt)‐based
conjugates,
thus
enabling
radiotherapy‐directed
chemotherapy.
Mechanistically,
irradiated
prodrugs
achieved
through
direct
photoelectron
transfer
from
excited‐state
nanoclusters
Pt(IV)
center,
resulting
release
cytotoxic
Pt(II)
agents.
Compared
traditional
combination
chemotherapy
and
radiotherapy,
this
offers
superior
antitumor
efficacy
safety
benefits
spatiotemporal
synergy
at
tumor
site.
Additionally,
elicits
robust
immunogenic
cell
death
yields
profound
outcomes
combined
immunotherapy
breast
cancer.
This
versatile
ushering
new
era
radiation‐mediated
chemistry
controlled
drug
delivery
precise
regulation
biological
processes.
Biochimica et Biophysica Acta (BBA) - Reviews on Cancer,
Год журнала:
2024,
Номер
1879(4), С. 189124 - 189124
Опубликована: Май 25, 2024
Apoptosis
has
traditionally
been
regarded
as
the
desired
cell
death
pathway
activated
by
chemotherapeutic
drugs
due
to
its
controlled
and
non-inflammatory
nature.
However,
recent
discoveries
of
alternative
pathways
have
paved
way
for
immune-stimulatory
treatment
approaches
in
cancer.
Ferroptosis
(dependent
on
iron)
cuproptosis
copper)
hold
promise
selective
cancer
targeting
overcoming
drug
resistance.
Copper
ionophores
iron-bearing
nano-drugs
show
potential
clinical
therapy
single
agents
adjuvant
treatments.
Here
we
review
up-to-date
evidence
involvement
metal
ion-dependent
cytotoxicity
classical
(alkylating
agents,
topoisomerase
inhibitors,
antimetabolites,
mitotic
spindle
inhibitors)
their
combinations
with
ferroptosis
inducers,
indicating
prospects,
advantages,
obstacles
use.
Cellular Oncology,
Год журнала:
2021,
Номер
44(5), С. 997 - 1017
Опубликована: Июль 27, 2021
HDAC9
(histone
deacetylase
9)
belongs
to
the
class
IIa
family
of
histone
deacetylases.
This
enzyme
can
shuttle
freely
between
nucleus
and
cytoplasm
promotes
tissue-specific
transcriptional
regulation
by
interacting
with
non-histone
substrates.
plays
an
essential
role
in
diverse
physiological
processes
including
cardiac
muscle
development,
bone
formation,
adipocyte
differentiation
innate
immunity.
inhibition
or
activation
is
therefore
a
promising
avenue
for
therapeutic
intervention
several
diseases.
overexpression
also
common
cancer
cells,
where
alters
expression
activity
numerous
relevant
proteins
involved
carcinogenesis.
