Unveiling the potential of isatin-grafted phenyl-1,2,3-triazole derivatives as dual VEGFR-2/STAT-3 inhibitors: Design, synthesis and biological assessments
Heba A. Elsebaie,
Maha-Hamadien Abdulla,
Zainab M. Elsayed
и другие.
Bioorganic Chemistry,
Год журнала:
2024,
Номер
151, С. 107626 - 107626
Опубликована: Июль 10, 2024
Язык: Английский
Identification of indole-grafted pyrazolopyrimidine and pyrazolopyridine derivatives as new anti-cancer agents: Synthesis, biological assessments, and molecular modeling insights
Bioorganic Chemistry,
Год журнала:
2024,
Номер
153, С. 107804 - 107804
Опубликована: Сен. 6, 2024
Язык: Английский
Synthesis and application of diazenyl sulfonamide-based schiff bases as potential BRCA2 active inhibitors against MCF-7 breast cancer cell line
Scientific Reports,
Год журнала:
2025,
Номер
15(1)
Опубликована: Фев. 24, 2025
In
this
study,
a
library
of
novel
sulfonamide-based
Schiff
bases
3a-j
was
synthesized
in
high
yield
(75
to
89%).
The
FTIR,
1H
NMR,
and
13C
NMR
spectroscopic
techniques
mass
analysis
were
used
characterize
the
compounds.
Their
anticancer
activity
assessed
vitro
on
breast
cancer
(MCF-7)
healthy
human
epithelial
(MCF-10
A)
cell
lines
over
48
72
h
using
MTT
assay.
Most
compounds
demonstrated
promising
activity,
with
compound
3i
showing
particularly
efficacy
at
(IC50
=
4.85
±
0.006
4.25
0.009
µM)
against
MCF-7
line.
Furthermore,
molecular
docking
studies
performed
for
PDB:
(3UV7)
protein
susceptibility
gene
2
(BRCA2).
obtained
results
revealed
that
has
strongest
binding
affinity
energy
(-7.99
kcal/mol),
consistent
experimental
data.
Additionally,
dynamics
(MD)
simulation
assays
confirm
formation
stable
3i-BRCA2
complex
strong
through
hydrogen
bonds.
Antioxidant
activities
determined
by
assay
DPPH
cation
radical
method.
Interestingly,
3j
12.36
0.55
had
comparable
ascorbic
acid
13.58
0.38
antioxidant
research
could
potentially
contribute
development
new
therapeutic
agents
useful
fighting
caused
cancer.
Язык: Английский
Discovery of 1-phenyl-1,2,3-triazole ureas as dual VEGFR-2/JNK-1 type II kinase inhibitors targeting pancreatic cancer
International Journal of Biological Macromolecules,
Год журнала:
2025,
Номер
unknown, С. 142372 - 142372
Опубликована: Март 1, 2025
Язык: Английский
Sulfonamides a Promising Hit for Cancer Therapy Through VEGFR-2 Inhibition
Biomedicines,
Год журнала:
2025,
Номер
13(4), С. 772 - 772
Опубликована: Март 21, 2025
Vascular
endothelial
growth
factor
receptor-2
(VEGFR-2),
a
tyrosine
kinase
receptor
(TKR),
plays
crucial
role
in
angiogenesis
and
is
overexpressed
most
cancers.
It
important
for
tumor
angiogenesis,
facilitating
essential
angiogenic
cellular
processes,
such
as
promoting
cell
survival,
proliferation,
migration,
vascular
permeability.
Consequently,
VEGFR-2
has
become
one
of
the
main
targets
anti-angiogenic
therapy,
with
its
inhibition
serving
strategy
developing
new
drugs
to
mitigate
angiogenesis-dependent
Small-molecule
targeting
VEGFR-2,
approved
by
USFDA,
are
exhibiting
development
drug
resistance
during
chemotherapy,
cardiac-related
side
effects
being
consistently
reported.
In
conclusion,
it
develop
novel
strategies
enhance
efficacy
inhibitors
eliminate
their
adverse
effects.
Multifunctional
that
target
multiple
pathways
present
promising
strategy,
enhancing
while
minimizing
Sulfonamide
derivatives
extensively
used
medicinal
chemistry
modern
discovery
due
variety
pharmacological
activities.
The
review
focuses
on
compounds
endowed
potential
inhibition,
four
which
additionally
carbonic
anhydrase
inhibitory
activity.
Язык: Английский
Discovery of new 1,3-diphenylurea appended aryl pyridine derivatives as apoptosis inducers through c-MET and VEGFR-2 inhibition: design, synthesis, in vivo and in silico studies
RSC Medicinal Chemistry,
Год журнала:
2024,
Номер
15(7), С. 2553 - 2569
Опубликована: Янв. 1, 2024
A
new
1,3-diphenylurea
appended
aryl
pyridine
derivative
was
designed,
synthesized
and
characterized
as
c-MET
VEGFR-2
inhibitors
to
induce
apoptosis
against
MCF-7
cells.
Язык: Английский
Fragment-based design and synthesis of coumarin-based thiazoles as dual c-MET/STAT-3 inhibitors for potential antitumor agents
Bioorganic Chemistry,
Год журнала:
2024,
Номер
151, С. 107682 - 107682
Опубликована: Авг. 6, 2024
Язык: Английский
Design and Discovery of New Dual Carbonic Anhydrase IX and VEGFR‐2 Inhibitors Based on the Benzenesulfonamide‐Bearing 4‐Thiazolidinones/2,4‐Thiazolidinediones Scaffold
Drug Development Research,
Год журнала:
2024,
Номер
85(8)
Опубликована: Дек. 1, 2024
Dual-targeting
drug
design
has
become
a
popular
approach
in
investigating
and
developing
potent
anticancer
agents.
In
this
regard,
carbonic
anhydrase
(CAIX)
vascular
endothelial
growth
factor
receptor
(VEGFR-2)
are
emerging
as
highly
effective
targets
the
battle
against
cancer.
present
study,
two
series
of
4-thiazolidinones/2,4-thiazolidinediones
carrying
2-methylbenzenesulfonamide
derivatives
were
designed
synthesized
potential
dual
CAIX/VEGFR-2
inhibitors.
All
target
compounds
evaluated
CAIX
enzyme
compared
to
dorzolamide
acetazolamide,
subsequently
most
inhibitors
(3a,
3b,
3o,
6d,
6g,
6i)
selected
evaluate
their
inhibitory
activity
VEGFR-2
using
sorafenib
reference
drug.
These
also
MCF-7
breast
cancer
cells
murine
fibroblast
3T3
cell
line.
According
results,
3b
(CAIX
IC
Язык: Английский