Chemistry - An Asian Journal,
Journal Year:
2022,
Volume and Issue:
18(3)
Published: Dec. 15, 2022
Abstract
We
report
a
palladium‐catalyzed
intramolecular
direct
heteroarylation
of
oxazole
tethered
β
‐naphthols
to
access
corresponding
tetracyclic
4
H
‐benzo[5,6]chromeno[3,4‐
d
]oxazoles.
Various
functional
groups
are
well
tolerated
and
furnished
the
desired
products
in
good
excellent
yields
under
present
reaction
conditions.
The
scale‐up
synthetic
utility
resulting
molecules
have
been
demonstrated.
Moreover,
UV/vis
absorption
fluorescence
emission
properties
evaluated
for
these
polyheterocyclic
compounds.
Phytomedicine,
Journal Year:
2024,
Volume and Issue:
129, P. 155600 - 155600
Published: April 7, 2024
Breast
cancer
stands
as
the
most
common
malignancy
among
women
globally
and
a
leading
cause
of
cancer-related
mortality.
Conventional
treatments,
such
surgery,
hormone
therapy,
radiotherapy,
chemotherapy,
small-molecule
targeted
often
fall
short
addressing
complexity
heterogeneity
certain
breast
subtypes,
to
drug
resistance
metastatic
progression.
Thus,
search
for
novel
therapeutic
targets
agents
is
imperative.
Given
their
low
toxicity
abundant
variety,
natural
products
derivatives
are
increasingly
considered
valuable
sources
anticancer
drugs.
This
review
aims
elucidate
pharmacological
impacts
underlying
mechanisms
active
compounds
found
in
select
derivatives,
primarily
focusing
on
treatment.
It
intends
underscore
potential
these
substances
combating
guide
future
research
directions
development
product-based
therapeutics.
We
conducted
comprehensive
searches
electronic
databases
PubMed,
Web
Science,
Scopus
until
October
2023,
using
keywords
'breast
cancer',
'natural
products',
'derivatives',
'mechanism',
'signaling
pathways',
various
keyword
combinations.
The
presents
spectrum
phytochemicals,
including
but
not
limited
flavonoids,
polyphenols,
alkaloids,
examines
actions
animal
cellular
models
cancer.
effects
manifested
through
diverse
mechanisms,
induction
cell
death
via
apoptosis
autophagy,
suppression
tumor
angiogenesis.
An
increasing
array
proving
effective
against
Future
strategies
can
benefit
from
strategic
enhancement
properties
compounds,
optimization
action,
improved
bioavailability,
minimized
side
effects.
forthcoming
should
prioritize
facets
maximize
Pharmaceuticals,
Journal Year:
2023,
Volume and Issue:
16(9), P. 1265 - 1265
Published: Sept. 6, 2023
The
importance
of
the
benzo[b]furan
motif
becomes
evident
in
remarkable
results
numerous
biological
investigations,
establishing
its
potential
as
a
robust
therapeutic
option.
This
review
presents
an
overview
synthesis
and
exhaustive
studies
conducted
on
derivatives
from
2011
to
2022,
accentuating
their
exceptional
promise
anticancer,
antibacterial,
antifungal
agents.
Initially,
discussion
focuses
chemical
synthesis,
molecular
docking
simulations,
both
vitro
vivo
studies.
Additionally,
we
provide
analysis
intricate
interplay
between
structure
activity,
thereby
facilitating
comparisons
profoundly
emphasizing
applications
within
realms
drug
discovery
medicinal
chemistry.
Journal of Advanced Research,
Journal Year:
2023,
Volume and Issue:
63, P. 219 - 230
Published: Nov. 1, 2023
Natural
products
(NPs)
play
a
crucial
role
in
the
development
of
therapeutic
drugs.
However,
it
is
still
highly
challenging
to
identify
targets
NPs.
Besides,
NPs
usually
exert
their
pharmacological
activities
via
acting
on
multiple
or
pathways,
which
also
poses
great
difficulties
for
target
identification
Journal of Medicinal Chemistry,
Journal Year:
2024,
Volume and Issue:
67(17), P. 14885 - 14911
Published: Aug. 16, 2024
As
an
obstinate
cancer
pancreatic
(PC)
poses
a
major
challenge
due
to
limited
treatment
options
which
include
resection
surgery,
radiation
therapy,
and
gemcitabine-based
chemotherapy.
In
cells,
protein
kinase
C
βI
(PKCβI)
participates
in
diverse
cellular
processes,
including
cell
proliferation,
invasion,
apoptotic
pathways.
the
present
study,
we
created
scaffold
develop
PKCβI
inhibitors
using
evodiamine-based
synthetic
molecules.
Among
candidate
inhibitors,
Evo312
exhibited
highest
antiproliferative
efficacy
against
PC
PANC-1,
acquired
gemcitabine-resistant
PANC-GR.
Additionally,
robustly
inhibited
activity.
Mechanistically,
effectively
suppressed
upregulation
of
expression,
leading
induction
cycle
arrest
apoptosis
PANC-GR
cells.
Furthermore,
exerted
antitumor
activity
cell-implanted
xenograft
mouse
model.
These
findings
position
as
promising
lead
compound
for
overcoming
gemcitabine
resistance
through
novel
mechanisms.
International Journal of Molecular Sciences,
Journal Year:
2023,
Volume and Issue:
24(7), P. 6021 - 6021
Published: March 23, 2023
Evodiamine
(EVO)
exhibits
anti-cancer
activity
through
the
inhibition
of
cell
proliferation;
however,
little
is
known
about
its
underlying
mechanism.
To
determine
whether
ferroptosis
involved
in
therapeutic
effects
EVO,
we
investigated
critical
factors,
such
as
lipid
peroxidation
levels
and
glutathione
peroxidase
4
(GPX4)
expression,
under
EVO
treatment.
Our
results
showed
that
inhibited
proliferation
poorly
differentiated,
high-grade
bladder
cancer
TCCSUP
cells
a
dose-
time-dependent
manner.
Lipid
peroxides
were
detected
by
fluorescence
microscopy
after
exposure
to
EVO.
GPX4,
which
catalyzes
conversion
prevent
from
undergoing
ferroptosis,
was
decreased
dose-dependently
Given
features
iron
dependency
lipid-peroxidation-driven
death
chelator
deferoxamine
(DFO)
used
suppress
EVO-induced
ferroptosis.
The
peroxide
level
significantly
when
treated
with
DFO
prior
also
attenuated
death.
Co-treatment
pan-caspase
inhibitor
or
necroptosis
did
not
alleviate
These
indicate
induces
rather
than
apoptosis
necroptosis.
Furthermore,
suppressed
migratory
ability,
expression
mesenchymal
markers,
increased
epithelial
marker
determined
transwell
migration
assay
Western
blotting.
tumor
xenograft
model
confirmed
on
growth
EMT.
In
conclusion,
novel
inducer
for
activating
may
be
potential
agent
cancer.
Journal of Medicinal Chemistry,
Journal Year:
2024,
Volume and Issue:
67(16), P. 14155 - 14174
Published: Aug. 6, 2024
Topoisomerase
(Top)
inhibitors
used
in
clinical
cancer
treatments
are
limited
because
of
their
toxicity
and
severe
side
effects.
Noteworthily,
Top1/2
dual
overcome
the
compensatory
effect
between
Top1
2
to
exhibit
stronger
antitumor
efficacies.
In
this
study,
a
series
indolo[3,2-
