Pharmaceutics,
Journal Year:
2021,
Volume and Issue:
13(6), P. 850 - 850
Published: June 8, 2021
Six
halogenated
trimethoxy
chalcone
derivatives
(CH1–CH6)
were
synthesized
and
spectrally
characterized.
The
compounds
further
evaluated
for
their
inhibitory
potential
against
monoamine
oxidases
(MAOs)
β-secretase
(BACE-1).
inhibited
MAO-B
more
effectively
than
MAO-A,
the
2′,3′,4′-methoxy
moiety
in
CH4–CH6
was
effective
inhibition
2′,4′,6′-methoxy
CH1–CH3.
Compound
CH5
most
potently
MAO-B,
with
an
IC50
value
of
0.46
µM,
followed
by
CH4
(IC50
=
0.84
µM).
In
(CH4-CH6),
order
–Br
>
-Cl
-F
CH6
at
para-position
ring
B
chalcone.
selective
selectivity
index
(SI)
values
15.1
31.3,
respectively,
over
MAO-A.
moderately
BACE-1
13.6
19.8
respectively.
When
assessed
cell
viability
studies
on
normal
African
Green
Monkey
kidney
line
(VERO)
using
MTT
assays,
it
noted
that
both
found
to
be
safe,
only
a
slightly
toxic
effect
observed
concentrations
above
200
µg/mL.
decreased
reactive
oxygen
species
(ROS)
levels
VERO
cells
treated
H2O2,
indicating
retained
protective
effects
antioxidant
activities.
All
showed
high
blood
brain
barrier
permeabilities
analyzed
parallel
artificial
membrane
permeability
assay
(PAMPA).
Molecular
docking
ADME
prediction
lead
provided
insights
into
rationale
behind
binding
CNS
drug
likeness.
From
non-test
mutagenicity
cardiotoxicity
studies,
non-mutagenic
non-/weak-cardiotoxic.
These
results
suggest
could
considered
candidates
cure
neurological
dysfunctions.
International Journal of Molecular Sciences,
Journal Year:
2021,
Volume and Issue:
22(21), P. 11306 - 11306
Published: Oct. 20, 2021
Cancer
is
a
condition
caused
by
many
mechanisms
(genetic,
immune,
oxidation,
and
inflammatory).
Anticancer
therapy
aims
to
destroy
or
stop
the
growth
of
cancer
cells.
Resistance
treatment
theleading
cause
inefficiency
current
standard
therapies.
Targeted
therapies
are
most
effective
due
low
number
side
effects
resistance.
Among
small
molecule
natural
compounds,
flavonoids
particular
interest
for
theidentification
new
anticancer
agents.
Chalcones
precursors
all
have
biological
activities.
The
activity
chalcones
ability
these
compounds
act
on
targets.
Natural
chalcones,
such
as
licochalcones,
xanthohumol
(XN),
panduretin
(PA),
loncocarpine,
been
extensively
studied
modulated.
Modification
basic
structure
in
order
obtain
with
superior
cytotoxic
properties
has
performed
modulating
aromatic
residues,
replacing
residues
heterocycles,
obtaining
hybrid
molecules.
A
huge
chalcone
derivatives
diaryl
ether,
sulfonamide,
amine
obtained,
their
presence
being
favorable
activity.
amino
group
aminochalconesis
always
antitumor
This
why
molecules
different
nitrogen
hetercycles
obtained.
From
these,
azoles
(imidazole,
oxazoles,
tetrazoles,
thiazoles,
1,2,3-triazoles,
1,2,4-triazoles)
importance
identification
Frontiers in Molecular Neuroscience,
Journal Year:
2023,
Volume and Issue:
15
Published: Jan. 4, 2023
Alzheimer's
disease
(AD)
is
a
common
age-related
neurodegenerative
characterized
by
progressive
cognitive
decline
and
irreversible
memory
impairment.
Currently,
several
studies
have
failed
to
fully
elucidate
AD's
cellular
molecular
mechanisms.
For
this
purpose,
research
on
related
models
may
propose
potential
predictive
for
the
drug
development
of
AD.
Therefore,
many
cells
neuronal
properties
are
widely
used
mimic
pathological
process
AD,
such
as
PC12,
SH-SY5Y,
N2a,
especially
PC12
pheochromocytoma
cell
line.
Thus,
review
covers
most
systematic
essay
that
study
We
depict
source,
culture
condition,
differentiation
methods,
transfection
drugs
inducing
general
approaches
(evaluation
methods
metrics),
in
vitro
parallel
with
cells.
BioMed Research International,
Journal Year:
2020,
Volume and Issue:
2020, P. 1 - 27
Published: July 3, 2020
Neurodegenerative
diseases
represent
nowadays
one
of
the
major
health
problems.
Despite
efforts
made
to
unveil
mechanism
leading
neurodegeneration,
it
is
still
not
entirely
clear
what
triggers
this
phenomenon
and
allows
its
progression.
Nevertheless,
accepted
that
neurodegeneration
a
consequence
several
detrimental
processes,
such
as
protein
aggregation,
oxidative
stress,
neuroinflammation,
finally
resulting
in
loss
neuronal
functions.
Starting
from
these
evidences,
there
has
been
wide
search
for
novel
agents
able
address
more
than
single
event
at
same
time,
so-called
multitarget-directed
ligands
(MTDLs).
These
compounds
originated
combination
different
pharmacophoric
elements
which
endowed
them
with
ability
interfere
enzymatic
and/or
receptor
systems,
or
exert
neuroprotective
effects
by
modulating
proteins
metal
homeostasis.
MTDLs
have
focus
latest
strategies
discover
new
treatment
Alzheimer’s
disease
(AD),
considered
most
common
form
dementia
characterized
cognitive
dysfunctions.
This
review
aimed
collecting
interesting
target
combinations
AD,
detailed
discussion
on
favorable
vitro
properties
optimized
structures
already
assessed
vivo
animal
models
dementia.
Pharmaceuticals,
Journal Year:
2022,
Volume and Issue:
15(12), P. 1560 - 1560
Published: Dec. 14, 2022
Alzheimer’s
disease
(AD)
is
a
neurodegenerative
disorder
characterized
by
decreased
synaptic
transmission
and
cerebral
atrophy
with
appearance
of
amyloid
plaques
neurofibrillary
tangles.
Cognitive,
functional,
behavioral
alterations
are
commonly
associated
the
disease.
Different
pathophysiological
pathways
AD
have
been
proposed,
some
which
interact
influence
one
another.
Current
treatment
for
mainly
involves
use
therapeutic
agents
to
alleviate
symptoms
in
patients.
The
conventional
single-target
approaches
do
not
often
cause
desired
effect
due
its
multifactorial
origin.
Thus,
multi-target
strategies
since
undertaken,
aim
simultaneously
target
multiple
targets
involved
development
AD.
In
this
review,
we
provide
an
overview
pathogenesis
current
drug
therapies
Additionally,
rationales
examples
drugs
pharmacological
actions
against
also
discussed.
Biosensors,
Journal Year:
2023,
Volume and Issue:
13(3), P. 359 - 359
Published: March 8, 2023
Throughout
this
research,
a
unique
optical
sensor
for
detecting
one
of
the
most
dangerous
heavy
metal
ions,
Cu(II),
was
designed
and
developed.
The
(4-mercaptophenyl)
iminomethylphenyl
naphthalenyl
carbamate
(MNC)
probe
effectively
prepared.
Schiff
base
shows
"turn-off"
state
with
excellent
sensitivity
to
Cu(II)
ions.
This
innovative
fluorescent
chemosensor
possesses
distinctive
features
substantial
Stocks
shift
(about
114
nm).
In
addition,
MNC
has
remarkable
selectivity
relative
other
cations.
Density
functional
theory
(DFT)
time-dependent
DFT
(TDDFT)
theoretical
calculations
were
performed
examine
chelation
structures
associated
electronic
properties
in
solution,
results
indicate
that
luminescence
quenching
complex
is
due
ICT.
Chelation-quenched
fluorescence
responsible
internal
charge
transfer
(ICT)-based
sensing
molecule
1:9
(v/v)
DMSO-HEPES
buffer
(20
mM,
pH
=
7.4)
Fluorescence
UV-Vis
absorption
ions
investigated.
By
utilizing
solution
containing
several
interference
studied.
outstanding
sensitivity,
as
well
low
LOD
(1.45
nM).
Consequently,
these
enable
it
find
copper
across
an
actual
narrow
dynamic
range
(0-1.2
M
Cu(II)).
reversibility
obtained
by
employing
EDTA
powerful
chelating
agent.
