Journal of Chemistry,
Год журнала:
2023,
Номер
2023, С. 1 - 17
Опубликована: Сен. 28, 2023
CuSO4/hydrazine
hydrate
was
used
as
a
catalyst
system
for
copper(I)-catalyzed
alkyne-azide
cycloaddition
(CuAAC)
of
AZT
and
5′-azido
adenosine
with
terminal
alkynes
to
give
30
novel
1,2,3-triazole
derivatives.
Screening
their
anticancer,
anti-inflammatory,
angiotensin-converting
enzyme
2
(ACE2),
3C-like
protease
(3CLpro)
inhibitory
activities
showed
that
several
triazoles
containing
murayafoline
A
indirubin-3′-oxime
inhibited
the
growth
HepG2
LU-1
IC50
values
ranging
from
11.01
19.87
μg/mL.
Besides
that,
some
triazole
derivatives
exhibited
anti-inflammatory
activity
against
RAW264.7
cells
within
an
interval
12.00–59.48.00
Especially,
two
at
O-
N1
positions
expressed
ACE2
3CLpro
in
which
both
135.62
142.95
μg/mL,
respectively.
Frontiers in Pharmacology,
Год журнала:
2021,
Номер
12
Опубликована: Окт. 26, 2021
Chemotherapy
is
the
most
common
clinical
treatment
for
non-small
cell
lung
cancer
(NSCLC),
but
low
efficiency
and
high
toxicity
of
current
chemotherapy
drugs
limit
their
application.
Therefore,
it
urgent
to
develop
hypotoxic
efficient
drugs.
Theophylline,
a
natural
compound,
safe
easy
get,
can
be
used
as
modified
scaffold
structure
hold
huge
potential
developing
antitumor
Herein,
we
linked
theophylline
with
different
azide
compounds
synthesize
new
type
1,2,3-triazole
ring-containing
derivatives.
We
found
that
some
theophylline1,2,3-triazole
showed
good
tumor-suppressive
efficacy.
Especially,
derivative
d17
strong
antiproliferative
activity
against
variety
cells
in
vitro,
including
H460,
A549,
A2780,
LOVO,
MB-231,
MCF-7,
OVCAR3,
SW480,
PC-9.
It
worth
noting
two
NSCLC
lines
H460
H
A549
are
sensitive
compound
particularly,
IC50
5.929
±
0.97
μM
6.76
0.25
μM,
respectively.
Compound
significantly
induce
apoptosis
by
increasing
ratio
apoptotic
protein
Bax/Bcl-2
downregulating
expression
phosphorylated
Akt
protein,
has
little
normal
hepatocyte
LO2
at
therapeutic
concentrations.
These
data
indicate
these
acetic
acid-1,2,3-triazole
derivatives
may
drug
candidates
anti-NSCLC
worthy
further
study.
Biointerface Research in Applied Chemistry,
Год журнала:
2021,
Номер
12(6), С. 8258 - 8270
Опубликована: Дек. 9, 2021
In
the
present
study,
1-(5-Methyl-1-(5-(methylthio)-1,3,4-thiadiazol-2-yl)-1H-1,2,3-triazol-4-yl)
ethan-1-one
2
was
used
as
predecessor
molecule
for
synthesis
of
methyl
2-(1-(5-methyl-1-(5-(methylthio)-1,3,4-thiadiazol-2-yl)-1H-1,2,3-triazol-4-yl)
ethylidene)
hydrazine-1-carbodithioate
3.
The
latter
compound
utilized
to
synthesize
two
new
1,3,4-thiadiazole-1,2,3-triazole
hybrids
6
and
7
via
its
reaction
with
appropriate
hydrazonoyl
halide
derivatives
4
5.
All
newly
prepared
derivatives'
chemical
composition
inferred
from
microanalytical
spectral
data
(FT-IR,
Mass
spectrometry,
1H-NMR,
13C-NMR).
Coronavirus
disease
(COVID-19)
is
an
infectious
that
can
cause
respiratory
tract
infections
humans
vertebrate
animals.
Herein,
we
reported
a
structure-aided
in
silico
virtual
screening
identify
their
antiviral
activity
against
through
inhibition
main
coronavirus
protease,
which
plays
essential
role
propagating
disease.
synthesized
compounds
showed
good
docking
scores
COVID-19
protease.
Journal of Chemistry,
Год журнала:
2023,
Номер
2023, С. 1 - 17
Опубликована: Сен. 28, 2023
CuSO4/hydrazine
hydrate
was
used
as
a
catalyst
system
for
copper(I)-catalyzed
alkyne-azide
cycloaddition
(CuAAC)
of
AZT
and
5′-azido
adenosine
with
terminal
alkynes
to
give
30
novel
1,2,3-triazole
derivatives.
Screening
their
anticancer,
anti-inflammatory,
angiotensin-converting
enzyme
2
(ACE2),
3C-like
protease
(3CLpro)
inhibitory
activities
showed
that
several
triazoles
containing
murayafoline
A
indirubin-3′-oxime
inhibited
the
growth
HepG2
LU-1
IC50
values
ranging
from
11.01
19.87
μg/mL.
Besides
that,
some
triazole
derivatives
exhibited
anti-inflammatory
activity
against
RAW264.7
cells
within
an
interval
12.00–59.48.00
Especially,
two
at
O-
N1
positions
expressed
ACE2
3CLpro
in
which
both
135.62
142.95
μg/mL,
respectively.
