International Journal of Molecular Sciences,
Год журнала:
2024,
Номер
25(22), С. 12401 - 12401
Опубликована: Ноя. 19, 2024
Breast
cancer
is
one
of
the
most
common
malignancies
affecting
women
worldwide,
with
a
significant
need
for
novel
therapeutic
agents
to
target
specific
molecular
pathways
involved
in
tumor
progression.
In
this
study,
series
rhodanine-piperazine
hybrids
were
designed,
synthesized,
and
evaluated
their
anticancer
activity,
targeting
key
tyrosine
kinases
such
as
VEGFR,
EGFR,
HER2.
Biological
screening
against
breast
cell
lines
(MCF-7,
MDA-MB-231,
T47D,
MDA-MB-468)
revealed
3
13
tested
compounds
potent,
5-({4-[bis(4-fluorophenyl)methyl]piperazin-1-yl}methylidene)-2-thioxo-1,3-thiazolidin-4-one
(
Future Medicinal Chemistry,
Год журнала:
2025,
Номер
17(3), С. 287 - 300
Опубликована: Янв. 17, 2025
New
phenyldiazene
scaffold-linked
heterocyclic
pyrazole,
pyrimidinone,
pyrimidinthione,
and/or
triazine
rings
have
been
developed
and
synthesized.
Cytotoxicity
of
our
derivatives
was
estimated
on
four
cancer
VERO
normal
cell
lines
targeting
EGFRT790M
(epidermal
growth
factor
receptor)
VEGFR-2
(vascular
endothelial
receptor-2)
enzymes.
Our
new
selectively
inhibited
both
EGFR
as
they
the
essential
structural
requirements
for
inhibitors
receptors.
Derivative
14
most
active
A549,
HCT116,
HepG2,
MCF-7
cancers
with
half-maximal
inhibitory
concentration
(IC50)
=
5.50,
9.77,
7.12,
7.85
µM
respectively.
The
assessed
5,
7,
8,
9,
10,
12
showed
IC50
54.40-62.60
μM
against
(normal
kidney)
cells
low
toxicity.
In
addition,
14,
7
9
were
discovered
to
be
very
good
at
values
1.15,
1.35,
140,
1.78
1.90
µM,
Furthermore,
strongly
repressed
0.28,
0.33,
0.35,
0.50
correspondingly.
Additionally,
highly
compounds
ADMET
profile.
could
considered
anticancer
agents
dual
inhibition.
RSC Advances,
Год журнала:
2023,
Номер
13(50), С. 35321 - 35338
Опубликована: Янв. 1, 2023
Novel
azobenzene
scaffold-joined
heterocyclic
isoxazole,
pyrazole,
triazole,
and/or
triazine
moieties
have
been
developed
and
synthesized
utilizing
microwave
traditional
methods.
Our
compounds
were
tested
for
growth
inhibition
of
A549,
MCF-7,
HCT-116,
HepG2
tumors
by
dual
targeting
the
VEGFR-2
EGFRT790M
enzymes.
The
suggested
compound's
manner
binding
with
active
sites
was
explored
through
molecular
design
MD
modeling.
information
from
results
biological
screening
docking
studies
highly
correlated.
A549
cell
line
one
that
responded
to
novel
effects
most
effectively.
Having
IC50
values
5.15,
6.37,
8.44
6.23
μM,
respectively,
14
effective
derivative
on
four
HCT116
cancer
cells.
It
had
greater
activity
than
erlotinib
slightly
inferior
activities
lines
sorafenib,
respectively.
cytotoxicity
derivatives,
5,
6,
10
14,
evaluated
against
typical
VERO
lines.
ranging
42.32
55.20
showed
investigated
drugs
modest
toxicity
normal
Additionally
all
derivatives
assessed
their
inhibitory
effects.
Among
them,
5
established
as
greatest
inhibitors
at
0.95,
1.25
1.50
μM
correspondingly.
As
well,
could
inhibit
demonstrating
strongest
=
0.25,
0.35,
0.40
0.50
Furthermore,
ADMET
profile
in
contrast
reference
sorafenib
erlotinib.
