Future Medicinal Chemistry,
Год журнала:
2023,
Номер
15(13), С. 1133 - 1147
Опубликована: Июль 1, 2023
Background:
Targeting
CDK4/6
has
advanced
breast
cancer
treatment.
Herein,
new
quinazolinones
were
synthesized
with
acetamide
linkers
as
potential
anti-breast
agents.
Methods
&
results:In
vitro
cytotoxic
evaluation
on
human
cell
lines
(MCF7
and
MDA-MB-231)
identified
1,3-benzodioxole
(5d)
to
be
of
the
highest
potency.
It
showed
good
inhibitory
activity
CDK4/6.
Compound
5d
arrested
cycle
at
G1-phase,
caused
induction
early
late
apoptosis
in
an
Annexin
V-FITC
assay,
led
increase
level
caspase-3
upregulated
Bax
expression
downregulated
Bcl-2
MCF7
cells.
radiosensitizing
when
combined
a
single
dose
8-Gy
γ-radiation.
Conclusion:
This
study
introduces
quinazolinone
scaffolds
inhibitors
for
cancer.
Phytomedicine,
Год журнала:
2024,
Номер
135, С. 155554 - 155554
Опубликована: Март 29, 2024
The
long
history
of
clinical
experience
in
China
have
confirmed
the
effectiveness
traditional
Chinese
medicine
(TCM)
treating
prostate
cancer
(PCa).
Until
now,
several
bioactive
compounds
with
anti-PCa
potential,
such
as
curcumin,
gallic
acid,
and
quercetin,
been
extracted
from
TCM.
Recent
studies
shown
that
encapsulating
these
TCM
into
nano-delivery
system
enhanced
their
bioavailability
improved
ability
to
target
PCa
tumors.
ACS Omega,
Год журнала:
2022,
Номер
7(26), С. 22639 - 22656
Опубликована: Июнь 23, 2022
To
discover
anticancer
drugs
with
novel
structures
and
expand
our
research
scope,
pyrazoline
derivatives
(3a-3l)
were
designed
synthesized
through
cyclization
of
chalcones
thiosemicarbazide/semicarbazide
in
CH3COOH
as
a
solvent.
All
newly
fully
characterized
using
several
spectroscopic
experiments
such
1H,
13C
NMR,
FT-IR
spectroscopy,
mass
analysis.
By
HPLC,
the
purity
all
analogs
was
found
above
95%
both
lead
compounds
(3a
3h)
also
validated
by
HRMS.
Anticancer
activity
investigated
MTT
assay
against
human
lung
cancer
cell
(A549),
cervical
(HeLa),
primary
normal
cells
(HFL-1).
Staurosporine
(STS)
used
standard
drug.
The
results
showed
that
two
potent
3a
3h
exhibit
excellent
A549
(IC50
=
13.49
±
0.17
22.54
0.25
μM)
HeLa
17.52
0.09
24.14
0.86
low
toxicity
HFL-1
114.50
0.01
173.20
10
μM).
flow
cytometry
further
to
confirm
line.
DNA
binding
interaction
agents
Ct-DNA
has
been
carried
out
absorption,
fluorescence,
EtBr
(dye
displacement
assay),
circular
dichroism,
cyclic
voltammetry
time-resolved
which
noncovalent
mode
interaction.
may
be
attributed
binding.
evaluation
antioxidant
potential
2,2-diphenyl-1-picrylhydrazyl
free
radical
promising
IC50
values
0.132
0.012
0.215
0.025
μg/mL,
respectively.
In
silico
molecular
docking
performed
autodock
vina
software
hexamer
PDB
ID:
1Z3F
ADMET
properties
explore
their
best
hits.
Molecules,
Год журнала:
2022,
Номер
27(19), С. 6632 - 6632
Опубликована: Окт. 6, 2022
Cancer
is
one
of
the
top
leading
causes
death
worldwide.
It
a
heterogenous
disease
characterized
by
unregulated
cell
proliferation
and
invasiveness
abnormal
cells.
For
treatment
cancer,
natural
products
have
been
widely
used
as
source
therapeutic
ingredients
since
ancient
times.
Although
compounds
their
derivatives
demonstrated
strong
antitumor
activity
in
many
types
poor
pharmacokinetic
properties,
low
selectivity,
limited
bioavailability
restricted
efficacy
against
drug-resistant
cancer
cells
hinder
wide
clinical
application.
Conjugation
with
other
bioactive
molecules
has
given
rise
to
new
field
drug
discovery
resulting
development
novel,
bifunctional
more
potent
drugs
for
therapy
overcome
current
drawbacks.
This
review
discusses
multiple
categories
such
conjugates
highlights
recent
trends
advances
product
hybrids.
Among
them,
ADCs,
PDCs,
ApDCs,
PROTACs
AUTOTACs
represent
emerging
agents
cancer.
Cell Communication and Signaling,
Год журнала:
2024,
Номер
22(1)
Опубликована: Апрель 11, 2024
Abstract
Cyclin-dependent
kinase
7
(CDK7)
serves
as
a
pivotal
regulator
in
orchestrating
cellular
cycle
dynamics
and
gene
transcriptional
activity.
Elevated
expression
levels
of
CDK7
have
been
ubiquitously
documented
across
spectrum
malignancies
concomitantly
correlated
with
adverse
clinical
outcomes.
This
review
delineates
the
biological
roles
explicates
molecular
pathways
through
which
exacerbates
oncogenic
progression
breast
cancer.
Furthermore,
we
synthesize
extant
literature
to
provide
comprehensive
overview
advancement
CDK7-specific
small-molecule
inhibitors,
encapsulating
both
preclinical
findings
cancer
contexts.
The
accumulated
evidence
substantiates
conceptualization
propitious
therapeutic
target
management.
Molecules,
Год журнала:
2022,
Номер
28(1), С. 277 - 277
Опубликована: Дек. 29, 2022
Traditional
methods
of
tumor
treatment
such
as
surgical
resection,
chemotherapy,
and
radiation
therapy
have
certain
limitations,
their
effects
are
not
always
satisfactory.
As
a
new
method,
photothermal
based
on
nanostructures
has
attracted
the
attention
researchers
due
to
its
characteristics
minimally
invasive,
low
side
effects,
inhibition
cancer
metastasis.
In
recent
years,
there
been
variety
inorganic
or
organic
used
in
field
treatment,
they
shown
great
application
prospects.
this
paper,
advantages
disadvantages
nanomaterials/nanostructures
agents
(PTAs)
for
well
research
progress
reviewed.
For
sake
clarity,
recently
reported
classified
into
five
main
categories,
i.e.,
carbon
nanostructures,
noble
metal
transition
sulfides,
polymer,
other
nanostructures.
addition,
future
perspectives
challenges
related
discussed.
