Archiv der Pharmazie,
Год журнала:
2025,
Номер
358(3)
Опубликована: Март 1, 2025
Abstract
Cancer,
with
its
steadily
increasing
morbidity
and
mortality,
will
continue
to
pose
a
threat
humanity
over
an
extended
period.
Chemotherapeutics
play
indispensable
role
in
cancer
treatment,
hundreds
of
drugs
have
been
approved
for
this
purpose.
Nevertheless,
the
fight
against
remains
formidable
challenge.
This
is
mainly
due
emergence
multidrug
resistance
severe
side
effects
associated
currently
available
anticancer
drugs.
Consequently,
there
urgent
imperative
explore
novel
chemotherapeutic
agents.
1,2,3‐Triazoles
belong
one
most
privileged
classes
nitrogen‐containing
five‐membered
heterocycles
are
regarded
as
prominent
sources
development
innovative
chemotherapeutics.
1,2,3‐Triazole
hybrids,
which
possess
multitargeted
mechanisms
action
within
progression
pathway,
hold
potential
overcome
mitigate
effects.
Furthermore,
several
1,2,3‐triazole
hybrids
already
therapy
or
under
clinical
evaluation.
clearly
demonstrates
that
valuable
scaffolds
treatment
eradication
cancer.
review
aims
provide
insights
into
therapeutic
along
their
action,
crucial
aspects
design,
structure–activity
relationships
(SARs).
It
encompasses
articles
published
from
2021
onward.
ACS Omega,
Год журнала:
2023,
Номер
8(7), С. 6669 - 6678
Опубликована: Фев. 13, 2023
Cancer
is
a
progressive
disease
that
frequently
encountered
worldwide.
The
incidence
of
cancer
increasing
with
the
changing
living
conditions
around
world.
side-effect
profile
existing
drugs
and
resistance
developing
in
long-term
use
increase
need
for
novel
drugs.
In
addition,
patients
are
not
resistant
to
bacterial
fungal
infections
due
suppression
immune
system
during
treatment.
Rather
than
adding
new
antibacterial
or
antifungal
drug
current
treatment
plan,
fact
anticancer
activity
has
these
effects
(antibacterial
antifungal)
will
patient's
quality
life.
For
this
purpose,
study,
series
10
naphthalene-chalcone
derivatives
were
synthesized
their
anticancer-antibacterial-antifungal
properties
investigated.
Among
compounds,
compound
2j
showed
against
A549
cell
line
an
IC50
=
7.835
±
0.598
μM.
This
also
activity.
apoptotic
potential
was
measured
by
flow
cytometry
14.230%.
58.870%
mitochondrial
membrane
potential.
Compound
inhibited
VEGFR-2
enzyme
0.098
0.005
Molecular
docking
studies
compounds
carried
out
silico
methods
caspase-3
enzymes.
Abstract
A
novel
series
of
1-(5-((6-nitroquinazoline-4-yl)thio)-1,3,4-thiadiazol-2-yl)-3-phenylurea
derivatives
8
were
designed
and
synthesized
to
evaluate
their
cytotoxic
potencies.
The
structures
these
obtained
compounds
thoroughly
characterized
by
IR,
1
H,
13
C
NMR,
MASS
spectroscopy
elemental
analysis
methods.
Additionally,
in
vitro
anticancer
activities
investigated
using
the
MTT
assay
against
A549
(human
lung
cancer),
MDA-MB231
triple-negative
breast
MCF7
hormone-dependent
cancer).
Etoposide
was
used
as
a
reference
marketed
drug
for
comparison.
Among
tested,
8b
8c
demonstrated
acceptable
antiproliferative
activity,
particularly
cells.
Considering
potential
VEGFR-2
inhibitor
potency
compounds,
molecular
docking
study
performed
most
potent
compound,
,
determine
its
probable
interactions.
Furthermore,
computational
investigations,
including
dynamics,
frontier
orbital
analysis,
Fukui
reactivity
descriptor,
electrostatic
surface,
silico
ADME
evaluation
all
illustrate
structure–activity
relationship
(SAR).
Future Medicinal Chemistry,
Год журнала:
2025,
Номер
17(4), С. 449 - 465
Опубликована: Янв. 31, 2025
The
study
of
chalcone-1,2,3-triazole
hybrids
for
anticancer
activity
is
quite
a
recent
area
focus,
primarily
because
the
increasing
demand
developing
new
drugs
to
treat
cancer.
chalcones
and
1,2,3-triazole
rings
in
hybrid
compounds
has
recently
emerged
as
promising
strategy
novel
agents.
ring,
known
its
stability
hydrogen
bonding
capabilities,
enhances
target
binding
affinity
these
hybrids.
Chalcones
possess
an
α,β-unsaturated
carbonyl
system
crucial
their
synergistic
effect
two
moieties
results
with
potent
properties.
This
review
explores
structure-activity
relationship
studies
which
revealed
that
electronic
lipophilic
properties
substituents
on
phenyl
significantly
influence
activity.
Electron-donating
electron-withdrawing
groups
can
affect
cellular
uptake
engagement.
Incorporating
various
into
ring
improve
selectivity
potency
against
specific
cancer
cell
lines.
These
often
exert
effects
through
apoptosis
cycle
disruption.
Recent
research
indicates
chalcone
hold
therapeutic
promise
Further
optimization
SAR
in-depth
mechanistic
investigations
could
lead
development
highly
selective
agents
minimal
toxicity.
Future Medicinal Chemistry,
Год журнала:
2025,
Номер
unknown, С. 1 - 15
Опубликована: Апрель 30, 2025
Breast
cancer
is
the
most
commonly
diagnosed
in
women
and
leading
cause
of
cancer-related
mortality
among
female
patients
across
world.
Chemotherapy
a
critical
means
for
breast
therapy,
administration
chemotherapy
could
reduce
risk
recurrence
by
approximately
one-third
early
cancer.
However,
multidrug
resistance
represents
principal
obstacle
to
effective
chemotherapeutic
interventions
against
an
increasing
clinical
challenge,
creating
urgent
demand
explore
innovative
chemotherapeutics
combat
this
formidable
disease.
Quinazoline
hybrids
with
structural
mechanistic
diversity
exhibit
excellent
activity
cancers
including
drug-resistant
forms
have
potential
side
effects
caused
corresponding
pharmacophores.
Notably,
lapatinib,
quinazoline-furan-sulfone
hybrid,
has
already
been
launched
therapy.
Thus,
quinazoline
represent
fertile
source
development
novel
deployment
control
eradication
This
review
emphasizes
current
scenario
antibreast
therapeutic
focuses
on
structure-activity
relationships
(SARs)
modes
action,
developed
from
2020
onwards,
facilitate
rational
discovery
more
candidates.
[Figure:
see
text]This
landscape
potential,
delves
into
mechanisms
action
aiming
less
toxic
Abstract
Cancer,
a
leading
global
cause
of
death,
necessitates
the
exploration
safer
and
more
effective
anticancer
drugs
due
to
adverse
side
effects
associated
with
current
cytotoxic
treatments.
Quinazoline
its
derivatives
have
emerged
as
promising
class
demonstrated
efficacy
against
diverse
tumor
types.
In
light
these
advancements,
this
comprehensive
review
aims
outline
recent
developments
in
utilization
quinazoline
agents.
Additionally,
article
offers
valuable
insights
into
potential
for
novel
serve
future
drugs.
By
delving
structure‐activity
relationship
study,
equips
researchers
thorough
understanding
necessary
designing
substantial
number
impactful
compounds,
which
hold
great
treatment
various
life‐threatening
disorders.
