Archiv der Pharmazie,
Год журнала:
2023,
Номер
356(8)
Опубликована: Май 21, 2023
Abstract
Despite
cancer
research
and
therapy,
breast
remains
a
complicated
health
crisis
in
women
represents
top
biomedical
priority.
Nowadays,
is
an
extremely
heterogeneous
disease
known
as
the
leading
cause
of
death
among
worldwide.
The
incidence
mortality
rates
have
been
increasing
gradually
for
past
decades.
common
treatments
are
chemotherapy,
endocrine
immunotherapy,
radiotherapy,
surgery.
most
targets
treatment
human
epidermal
growth
factor
receptor
2
(HER2)
estrogen
receptors.
literature
suggests
that
several
targets/pathways
also
involved
development
cancer,
is,
poly(ADP‐ribose)
polymerase
(PARP),
bromodomain‐containing
protein
4
(BRD4),
cyclin‐dependent
kinase
4/6
(CDK4/6),
(EGFR),
vascular
endothelial
(VEGFR),
polo‐like
1
(PLK1),
phosphoinositide
3‐kinases/protein
B/mammalian
target
rapamycin
(PI3K/AKT/mTOR),
histone
deacetylase
(HDAC),
nuclear
kappa
B
(NF‐κB),
PD‐L1,
aromatase
inhibitors.
Meanwhile,
study
hot
topic
current
scenario
basic/clinical
research.
This
review
article
provides
information
on
different
associated
with
summarizes
progress
synthesized
inhibitors
anti‐breast
agents
from
2015
to
2021.
aims
provide
structure–activity
relationship
docking
studies
designing
novel
compounds
therapy.
Future Medicinal Chemistry,
Год журнала:
2024,
Номер
16(14), С. 1449 - 1464
Опубликована: Май 30, 2024
Aim:
This
study
explores
the
cytotoxic
and
apoptotic
effects
of
novel
thiazolidinone-1,2,3-triazole
hybrids
on
HT-1080,
A-549,
MDA-MB-231
cancer
cell
lines.
Methods
&
results:
The
synthesized
compounds
underwent
comprehensive
characterization
(NMR
HRMS)
to
confirm
their
structures
purity.
Subsequent
anticancer
activity
screening
across
diverse
lines
revealed
promising
antitumor
potential
notably,
6f
6g.
Mechanistic
investigations
unveiled
that
compound
triggers
apoptosis
through
caspase-3/7
pathway.
In
terms
in
silico
studies,
was
identified
as
a
potent
inhibitor
caspase-3
caspase-7.
Conclusion:
present
underscores
therapeutic
against
certain
cells.
These
findings
highlight
avenue
for
development
treatment
strategies
utilizing
these
(R)-Carvone-based
derivatives.
ACS Omega,
Год журнала:
2023,
Номер
8(43), С. 40287 - 40298
Опубликована: Окт. 19, 2023
Breast
cancer
remains
a
challenging
medical
issue
and
is
high
priority
for
biomedical
research
despite
significant
advancements
in
therapy.
The
current
study
aims
to
determine
the
anticancer
activity
of
group
imidazole-pyridine-based
scaffolds
against
variety
breast
cell
lines
differing
their
receptor
expression
(estrogen
(ER),
progesterone
(PR),
HER-2).
A
series
10
molecules
(coded
5a-5j)
were
synthesized
through
multicomponent
alkylation
reactions.
FTIR,
MS,
1H,
13C
NMR
spectral
analyses
confirmed
structures
purity
molecules.
Subsequently,
these
tested
ability
inhibit
viability
representing
carcinoma
breast,
viz.,
MDA-MB-468
(ER-,
PR-,
HER-),
BT-474
(ER+,
PR+,
HER+),
T-47D
MCF-7
HER-)
vitro.
Among
molecules,
5a,
5c,
5d,
5e
exhibited
better
potency,
as
evidenced
by
IC50
<
50
μM
at
24
h
treatment
lines.
However,
except
value
much
higher
than
when
T47D
24h.
Extended
48
reduced
effect
an
increase
was
observed.
In
mice,
intraperitoneal
administration
retarded
Ehrlich
ascites
(EAC)
growth
without
causing
any
organ
toxicity
doses
tested.
summary,
we
report
synthesis
scheme
key
structural
requirements
new
imidazole-pyridine
vitro
inhibition
feasibility
cells
vivo
EAC
tumors.
Biomedicines,
Год журнала:
2024,
Номер
12(6), С. 1192 - 1192
Опубликована: Май 27, 2024
Breast
cancer
is
the
most
common
among
women.
Currently,
it
poses
a
significant
threat
to
healthcare
system
due
emerging
resistance
and
toxicity
of
available
drug
candidates
in
clinical
practice,
thus
generating
an
urgent
need
for
development
new
potent
safer
anti-breast
candidates.
Coumarin
(chromone-2-one)
elite
ring
widely
distributed
natural
products
possesses
broad
range
pharmacological
properties.
The
unique
distribution
efficacy
coumarins
attract
product
hunters,
resulting
identification
numerous
from
different
sources
last
three
decades,
especially
those
with
Inspired
by
this,
synthetic
derivatives
based
on
have
been
developed
medicinal
chemists
all
around
globe,
showing
promising
efficacy.
This
review
primarily
focused
coumarin-inspired
agents
highlighting
design
strategies,
mechanistic
insights,
their
structure–activity
relationship.
Natural
having
are
also
briefly
highlighted.
will
act
as
guideline
researchers
designing
optimum
coumarin-based
agents.
Scientific Reports,
Год журнала:
2022,
Номер
12(1)
Опубликована: Дек. 31, 2022
Adjuvant
endocrine
therapy
improves
the
prognosis
of
early
breast
cancer
with
hormone
receptor
positivity.
However,
there
is
no
systematic
report
on
effect
(particularly
ovarian
function
suppression,
OFS)
serum
lipids
in
premenopausal
women.
This
retrospective
cohort
study
aimed
to
determine
whether
various
treatments
had
different
effects
blood
lipids.
enrolled
160
patients
stage
I-III
eastern
China.
The
initial
diagnostic
information
was
retrieved
from
patient's
medical
records,
including
age
at
time
diagnosis,
tumor
characteristics,
anticancer
treatment
and
past
history.
changes
receiving
types
were
compared
3rd,
6th,
12th,
24th
months
after
initiating
therapy.
Generalized
linear
mixed
model
used
our
analyses.
Our
data
revealed
that
low-density
lipoprotein
cholesterol
(LDL-C)
levels
tamoxifen
(TAM)
significantly
lower
than
3rd
month,
while
high-density
(HDL-C)
higher
indicating
lipid
generally
improved
time.
While
TAM
plus
OFS
group,
HDL-C
month
total
(TC)
6th
month.
profiles
aromatase
inhibitor
(AI)
group
did
not
show
significant
differences
any
point
but
those
other
two
groups
especially
LDL
TC.
tended
have
levels.
With
longer
follow-up,
statistically
difference
values
observed
between
points.
Compared
groups,
AI
presented
an
increasing
trend
toward
LDL-C
risk
dyslipidemia
requires
further
investigation
using
a
large
sample
size.
New Journal of Chemistry,
Год журнала:
2023,
Номер
47(24), С. 11602 - 11614
Опубликована: Янв. 1, 2023
A
set
of
1,2,4-triazoles
containing
a
hydrazone
moiety
was
synthesized
by
oxidative
cyclization
utilizing
molecular
iodine
under
mild
conditions.
These
compounds
were
evaluated
as
anticancer
agents
and
their
binding
mechanism
investigated.
