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.
RSC Advances,
Год журнала:
2022,
Номер
12(41), С. 26895 - 26907
Опубликована: Янв. 1, 2022
An
essential
target
for
COVID-19
is
the
main
protease
of
SARS-CoV-2
(Mpro).
With
objective
targeting
this
receptor,
a
novel
set
pyrido[1,2-a]pyrrolo[2,3-d]pyrimidines
with
terminal
carboxamide
fragments
was
designed,
synthesized,
and
considered
as
an
initial
motif
creation
effective
pan-coronavirus
inhibitors.
Accordingly,
nine
derivatives
(21-29)
have
been
introduced
in
vitro
assay
to
evaluate
their
antiviral
activity
cytotoxicity
effect
against
virus
using
Vero
cells.
The
obtained
data
revealed
that
majority
these
showed
potent
cellular
anti-COVID-19
prevent
viral
growth
by
more
than
90%
at
two
different
concentrations
weak
or
even
no
detectable
cytotoxic
on
Extensive
molecular
docking
simulations
highlighted
proper
non-covalent
interaction
new
compounds
within
binding
pocket
Mpro
potential
activity.
In
all
synthesized
indicated
25
29
promising
inhibitory
IC50
values
low
micromolar
concentrations.
dynamic
simulation
results
predicted
stability
compound
cavity
hence
supported
high
shown
assay.
These
suggested
merit
further
investigations
drug
candidates
management
SARS-CoV-2.
Pharmaceuticals,
Год журнала:
2023,
Номер
16(3), С. 463 - 463
Опубликована: Март 20, 2023
COVID-19
infection
is
now
considered
one
of
the
leading
causes
human
death.
As
an
attempt
towards
discovery
novel
medications
for
pandemic,
nineteen
compounds
containing
1,2,3-triazole
side
chains
linked
to
phenylpyrazolone
scaffold
and
terminal
lipophilic
aryl
parts
with
prominent
substituent
functionalities
were
designed
synthesized
via
a
click
reaction
based
on
our
previous
work.
The
assessed
using
in
vitro
effect
growth
SARS-CoV-2
virus-infested
Vero
cells
different
compound
concentrations:
1
10
μM.
data
revealed
that
most
these
derivatives
showed
potent
cellular
anti-COVID-19
activity
inhibited
viral
replication
by
more
than
50%
no
or
weak
cytotoxic
harboring
cells.
In
addition,
assay
employing
SARS-CoV-2-Main
protease
inhibition
was
done
test
inhibitors'
ability
block
common
primary
virus
as
mode
action.
obtained
results
show
non-linker
analog
6h
two
amide-based
linkers
6i
6q
active
IC50
values
5.08,
3.16,
7.55
μM,
respectively,
against
comparison
selective
antiviral
agent
GC-376.
Molecular
modeling
studies
placement
within
binding
pocket
which
reveal
conserved
residues
hydrogen
bonding
non-hydrogen
interactions
fragments:
triazole
scaffold,
part,
linker.
Moreover,
stability
their
target
also
studied
analyzed
molecular
dynamic
simulations.
physicochemical
toxicity
profiles
predicted,
behave
low
organ
toxicity.
All
research
point
potential
usage
new
chemotype
promising
leads
be
explored
vivo
might
open
door
rational
drug
development
Main
medicines.
Molecules,
Год журнала:
2023,
Номер
28(10), С. 4009 - 4009
Опубликована: Май 10, 2023
Chalcones
are
direct
precursors
in
the
biosynthesis
of
flavonoids.
They
have
an
α,β-unsaturated
carbonyl
system
which
gives
them
broad
biological
properties.
Among
properties
exerted
by
chalcones,
their
ability
to
suppress
tumors
stands
out,
addition
low
toxicity.
In
this
perspective,
present
work
explores
role
natural
and
synthetic
chalcones
anticancer
activity
vitro
reported
last
four
years
from
2019
2023.
Moreover,
we
carried
out
a
partial
least
square
(PLS)
analysis
biologic
data
for
colon
adenocarcinoma
lineage
HCT-116.
Information
was
obtained
Web
Science
database.
Our
silico
identified
that
presence
polar
radicals
such
as
hydroxyl
methoxyl
contributed
derivatives.
We
hope
presented
will
help
researchers
develop
effective
drugs
inhibit
future
works.
