Design, synthesis, and antiproliferative screening of new quinoline derivatives bearing a cis-vinyl triamide motif as apoptosis activators and EGFR-TK inhibitors
Hany M. Abd El‐Lateef,
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Ahmed Gaafar Ahmed Gaafar,
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Arwa Sultan Alqahtani
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et al.
RSC Advances,
Journal Year:
2024,
Volume and Issue:
14(34), P. 24781 - 24790
Published: Jan. 1, 2024
A
set
of
novel
quinoline
tethered
cis
-vinyl
triamides
derivatives
has
been
designed,
synthesized
and
screened
for
in
vitro
cytotoxicity
against
the
MCF-7
breast
adenocarcinoma
cell
line.
Language: Английский
Synthesis and biological research of new imidazolone-sulphonamide-pyrimidine hybrids as potential EGFR-TK inhibitors and apoptosis-inducing agents
RSC Advances,
Journal Year:
2024,
Volume and Issue:
14(28), P. 20120 - 20129
Published: Jan. 1, 2024
Development
of
new
effective
EGFR-targeted
antitumor
agents
is
needed
because
their
clinical
significance.
A
series
imidazolone-sulphonamide-pyrimidine
hybrids
was
designed
and
synthesized
as
modified
analogs
some
reported
EGFR
inhibitors.
The
cytotoxic
activity
all
the
investigated
against
breast
MCF-7
cancerous
cell
line
using
doxorubicin
(Dox)
a
positive
control.
4-(Furan-2-ylmethylene)imidazolone-sulphonamide-pyrimidine
6b
had
best
potent
cells
with
IC50
result
1.05
μM,
which
better
than
Dox
(IC50
=
1.91
μM).
In
addition,
mechanistic
studies
revealed
ability
compounds
5g,
5h
to
inhibit
kinase.
Cell
cycle
analysis
that
compound
can
halt
at
G1
phase
concomitant
decrease
in
cellular
percentage
S
G2/M
phases.
This
produced
noticeable
rise
proportion
apoptotic
regard
untreated
Furthermore,
effects
hybrid
on
expression
levels
pro-apoptotic
Bax
pro-survival
Bcl2
were
assessed.
results
showed
this
upregulated
level
well
declined
value
Bcl-2
Language: Английский
Synthesis, characterization and biological research of novel 2-(quinoline-4-carbonyl)hydrazide-acrylamide hybrids as potential anticancer agents on MCF-7 breast carcinoma cells by targeting EGFR-TK
RSC Advances,
Journal Year:
2024,
Volume and Issue:
14(32), P. 23495 - 23504
Published: Jan. 1, 2024
A
sequence
of
novel
2-(quinoline-4-carbonyl)hydrazide
scaffolds
carrying
the
acrylamide
moiety
have
been
synthesized
and
evaluated
for
in
vitro
cytotoxicity
against
an
MCF-7
breast
cancer
cell
line.
Language: Английский
Novel Quinolin-4-ylcarbonylhydrazine Having N-(3-Arylacryloyl) Moiety: Design, Synthesis and Biological Evaluation as Potential Cytotoxic Agents against MDA-MB-231 via Tubulin Assembly Inhibition
Journal of Molecular Structure,
Journal Year:
2024,
Volume and Issue:
1321, P. 140214 - 140214
Published: Sept. 27, 2024
Language: Английский
Design and synthesis of novel 2-(2-(4-bromophenyl)quinolin-4-yl)-1,3,4-oxadiazole derivatives as anticancer and antimicrobial candidates: in vitro and in silico studies
RSC Advances,
Journal Year:
2024,
Volume and Issue:
14(46), P. 34005 - 34026
Published: Jan. 1, 2024
Cancer
is
the
second
leading
cause
of
death
globally,
surpassed
only
by
heart
disease.
Moreover,
bacterial
infections
remain
a
significant
global
health
burden,
contributing
substantially
to
morbidity
and
mortality,
especially
among
hospitalized
patients.
EGFR
has
emerged
as
prime
therapeutic
target
due
its
pivotal
role
in
driving
uncontrolled
cell
growth
survival
across
numerous
cancer
types.
In
addition,
DNA
gyrase
represents
promising
for
development
novel
antimicrobial
agents.
Therefore,
we
aimed
design
synthesize
new
multi-target
quinoline
hybrids
(7-17e)
capable
acting
anti-proliferative
agents
inhibiting
microbial
gyrase,
respectively.
The
inhibitory
potential
synthesized
compounds
was
determined
using
Language: Английский