Materials Express,
Journal Year:
2023,
Volume and Issue:
13(12), P. 2110 - 2127
Published: Nov. 14, 2023
Five
manufactured
mixed
ligands
chelate
of
Schiff
base
(HL)
in
the
presence
8-hydroxyquinoline
(HQ)
with
Chromium(III),
Cobalt(II),
Silver(I)
tin(II),
and
mercury(II)
was
produced
described.
The
molecular
structure
complexes
examined
using
physicochemical
analysis,
thermogravimetric
spectroscopic
methods.
Measurements
morphological
properties
confirm
nano-crystalline
particles
fabricated
chelates.
FT-IR
analysis
revealed
that
HL
HQ
chelated
metal
ions
as
NO
bi-dentate
ligands.
synthesized
have
distorted
octahedral
(Cr(III)
Co(II))
tetrahedral
(Ag(I),
Sn(II),
Hg(II)
forms,
according
to
magnetic
electronic
spectrum
data.
Thermogravimetric
(TG)
indicates
formation
were
stable.
antimicrobial
antiviral
effectiveness
their
has
also
been
investigated.
results
indicated
newly
prepared
greater
activity
contrast
free
ligands,
Studies
on
docking
performed
out
order
determine
optimal
engagement
location
well
its
inhibitory
activity.
Journal of Medicinal Chemistry,
Journal Year:
2023,
Volume and Issue:
66(8), P. 5550 - 5566
Published: April 3, 2023
A
proposed
strategy
to
overcome
multidrug
resistance
(MDR)
of
anticancer
drugs
in
chemotherapy
is
disable
the
efflux
function
P-glycoprotein
(P-gp).
In
this
study,
based
on
ring-merging
and
fragment-growing
strategies,
105
novel
benzo
five-membered
heterocycle
derivatives
were
designed,
synthesized,
screened.
Exploration
structure-activity
relationship
(SAR)
led
identification
d7
with
low
cytotoxicity
promising
reversal
activity
doxorubicin
MCF-7/ADR
cells.
Furthermore,
mechanism
studies
revealed
that
stemmed
from
inhibition
P-gp
efflux.
Molecular
docking
further
clarified
observed
trends
SAR
displaying
potent
affinity
P-gp.
Additionally,
coadministration
achieved
stronger
antitumor
a
xenograft
model
than
alone.
These
results
suggest
potential
MDR
reveal
agent
acting
as
inhibitor
provides
guidelines
for
future
development
new
inhibitors.
ACS Chemical Neuroscience,
Journal Year:
2024,
Volume and Issue:
15(7), P. 1388 - 1414
Published: March 25, 2024
Alzheimer's
disease
(AD)
is
the
most
common
cause
of
dementia,
which
arises
due
to
low
levels
acetyl
and
butyrylcholines,
an
increase
in
oxidative
stress,
inflammation,
metal
dyshomeostasis,
Aβ
tau
aggregations.
The
currently
available
drugs
for
AD
treatment
can
provide
only
symptomatic
relief
without
interfering
with
pathological
hallmarks
disease.
In
our
ongoing
efforts
develop
naturally
inspired
novel
multifunctional
molecules
AD,
systematic
SAR
studies
on
EJMC-4e
were
caried
out
improve
its
properties.
rigorous
medicinal
led
development
12o,
displayed
a
15-fold
enhancement
antioxidant
properties
2-fold
activity
against
AChE
BChE
over
EJMC-4e.
Molecular
docking
dynamics
revealed
binding
sites
stability
complex
12o
BChE.
PAMPA-BBB
assay
clearly
demonstrated
that
easily
cross
blood–brain
barrier.
Interestingly,
also
expresses
promising
chelation
activity,
while
was
found
be
devoid
this
property.
Further,
inhibited
metal-induced
or
self
Aβ1–42
aggregation.
Observing
neuroprotection
ability
H2O2-induced
stress
PC-12
cell
line
noteworthy.
Furthermore,
NLRP3
inflammasome
activation
attenuated
mitochondrial-induced
ROS
MMP
damage
caused
by
LPS
ATP
HMC-3
cells.
addition,
able
effectively
reduce
mitochondrial
cellular
Drosophila
model.
Finally,
could
reverse
memory
impairment
scopolamine-induced
mice
model,
as
evident
through
vivo
ex
studies.
These
findings
suggest
compound
may
act
candidate
further
improvement
management
AD.
Journal of Medicinal Chemistry,
Journal Year:
2024,
Volume and Issue:
67(16), P. 13909 - 13924
Published: Aug. 2, 2024
Multidrug
resistance
(MDR)
of
human
tumors
has
resulted
in
an
immediate
need
to
develop
appropriate
new
drugs.
This
work
outlines
the
development
20
potent
IQQ
N-oxide
derivatives
two
isomeric
families,
both
exhibiting
nanomolar
GI50
against
tumor
cell
lines.
Preliminary
NCI-60
screening
sees
C(6)
isomers
achieve
a
mean
>
2
times
lower
than
corresponding
C(7)
isomers.
MDR
evaluation
nine
selected
compounds
reveals
that
each
presents
concentrations
Four
series
display
values
cells,
having
selectivity
ratios
up
2.7
versus
sensitive
(parental)
cells.
The
most
compound
25
inhibits
activity
drug
efflux
pumps
causes
significant
ROS
accumulation,
and
potently
proliferation,
causing
alterations
cycle
profile.
Our
findings
are
confirmed
by
3D
spheroid
models,
providing
candidates
for
studies
cancers.
Journal of Medicinal Chemistry,
Journal Year:
2025,
Volume and Issue:
unknown
Published: Feb. 27, 2025
A
series
of
marchantin
C-NO
donor
hybrids
were
designed,
synthesized,
and
evaluated
for
their
antitumor
activity
in
vitro
vivo.
Notably,
MC-furoxan
hybrid
14
exhibited
the
best
selective
inhibitory
against
MCF-7/ADR
(IC50
=
0.024
μM)
with
883
times
potency
compared
MCF-7
cells
21.20
μM),
cytotoxicity
toward
A549/Taxol
1.43
increased
17-fold
that
A549
23.75
μM).
Preliminary
pharmacological
studies
revealed
could
"hijack"
lysosomal
Pgp
release
NO
to
produce
reactive
oxygen
species
(ROS)
lysosomes,
resulting
membrane
permeabilization
(LMP)
potentiated
cytotoxicity.
Additionally,
compound
achieved
stronger
superior
biosafety
at
relatively
low
doses
than
paclitaxel
xenograft
model.
In
summary,
this
study
provides
a
promising
strategy
design
such
like
overcome
MDR
via
utilization
transport
activity.
