Design and synthesis of novel pyrimidine-pyrazole hybrids with dual anticancer and anti-inflammatory effects targeting BRAFV600E and JNK
Molecular Diversity,
Journal Year:
2025,
Volume and Issue:
unknown
Published: Feb. 22, 2025
Abstract
Two
new
series
of
pyrimidinyl
ethyl
pyrazoles
derivatives
13a–f
and
14a–f
were
designed
synthesized
to
possess
both
anticancer
effect
by
inhibiting
BRAFV600E
anti-inflammatory
JNK
isoforms.
The
structure
the
compounds
was
generated
from
hybridization
two
main
moieties.
moiety
reported
inhibitors,
pyrazole
isoforms
inhibitors.
final
tested
on
BRAFV600E,
JNK1,
JNK2,
JNK3
measure
their
kinases
inhibitory
effect.
Compound
14c
showed
highest
activity
with
IC
50
=
0.51
μM,
0.53
1.02
0.009
μM
JNK3,and
respectively.
All
over
four
cancer
cell
lines
related
target
enzymes.
14d
most
potent
all
0.87
0.91,
0.42
0.63
MOLT-4,
K-562,
SK-MEL-28,
A375
lines,
ability
inhibit
MEK1/2
ERK1/2
phosphorylation
performed
using
western
blot.
cycle
analysis
compound
line
revealed
that
arrested
growth
at
G0-G1
phase.
remarkably
decreased
migration
compared
control
group
in
traditional
test.
Compounds
significant
nitric
oxide
release
PGE2
production
raw
264.7
macrophages.
13d
1
4d
exhibited
high
iNOS
COX-2
COX-1.
Finally,
TNF-alpha
IL-6
determined.
Graphical
abstract
synthesized.
able
BRAFV600E.
play
a
key
role
inflammatory
disorders.
Final
for
activities.
Language: Английский
Design and synthesis of novel cyclohexanecarboxamides with anticonvulsant effect by activating Nrf2-ARE pathway
Bioorganic Chemistry,
Journal Year:
2025,
Volume and Issue:
159, P. 108357 - 108357
Published: March 10, 2025
Language: Английский
Search for New Compounds with Anti-Inflammatory Activity Among 1,2,4-Triazole Derivatives
Teresa Glomb,
No information about this author
Joe O. Minta,
No information about this author
Michalina Nowosadko
No information about this author
et al.
Molecules,
Journal Year:
2024,
Volume and Issue:
29(24), P. 6036 - 6036
Published: Dec. 21, 2024
Compounds
containing
the
1,2,4-triazole
moiety
in
their
structure
exhibit
broad
biological
activities.
Many
of
these
compounds
demonstrate
anti-inflammatory
activity
vitro
through
various
mechanisms,
such
as
inhibiting
COX-1/COX-2
and
LOX,
modulating
pro-inflammatory
cytokine
levels,
or
having
effects
on
other
specific
enzymes.
Some
also
display
activities
vivo.
In
many
publications,
new
1,2,4-triazole-based
exceed
those
reference
drugs,
suggesting
promising
potential
therapeutic
agents.
This
review
active
derivatives
with
is
based
literature
published
from
2015–2024.
Language: Английский