Chemistry & Biodiversity,
Journal Year:
2024,
Volume and Issue:
21(12)
Published: Aug. 23, 2024
Abstract
Chalcone‐incorporated
pyridine‐pyrimidines
i.e.
derivatives
of
(5‐(6‐(pyrimidin‐5‐yl)pyridin‐3‐yl)thiophen‐2‐yl)prop‐2‐en‐1‐one
were
synthesized
and
their
structures
confirmed
by
analytical
techniques.
In
addition,
all
the
examined
for
capacity
to
fight
against
cancer
towards
four
cell
lines,
including
breast
(MCF‐7),
prostate
(DU‐145
PC3),
lung
(A549)
utilizing
MTT
technique
clinically
used
chemotherapy
medication,
etoposide
serving
as
a
positive
reference.
All
these
results
expressed
in
IC
50
μM,
values
compounds
are
compared
with
reference
drug,
showing
ranging
from
1.97±0.45
μM
3.08±0.135
μM.
Among
those,
few
10(a–e
)
demonstrated
strong
activities
corresponding
lines.
ChemistrySelect,
Journal Year:
2025,
Volume and Issue:
10(15)
Published: April 1, 2025
Abstract
The
highly
increased
and
global
mortality
due
to
cancer
has
created
an
urgent
need
discover
promising
targets
for
its
treatment.
Where
drug
repurposing
was
considered
as
attractive
approach
that
can
facilitate
the
lead
generation
optimization
phases
of
discovery
by
existing
agents
target
diseases
other
than
their
primary
uses.
Cheminformatics
studies
represented
in
molecular
docking
well
dynamic
simulation
salicylic
acid
/
aspirin
analogues
sulindac
indomethacin
anti‐inflammatory
drugs
were
carried
out
be
used
cyclin‐dependent
kinases
(CDKs)
namely
CDK2,
CDK6,
CDK12
inhibitors.
Sulindac
displayed
best
binding
ligand
all
receptors.
CDKs
inhibition
effects
three
sulindac,
anthranilic
demonstrated
good
inhibitory
activity
against
ranging
from
0.48
1.78
µM.
Likewise,
cytotoxicity
revealed
potent
anticancer
0.155
1.278
µM
cell
lines:
HCT‐116,
MCF‐7,
HeLa
cells.
As
a
result,
this
technique
saves
lot
time
money
order
new
agents.
Molecules,
Journal Year:
2024,
Volume and Issue:
29(2), P. 346 - 346
Published: Jan. 10, 2024
Aromatase
is
an
enzyme
that
plays
a
crucial
role
in
the
biosynthesis
of
estrogens,
which
are
hormones
contribute
to
growth
certain
types
breast
cancer.
In
particular,
aromatase
catalyzes
conversion
androgens
(male
hormones)
into
estrogens
(female
various
tissues,
including
adrenal
glands,
ovaries,
and
adipose
tissue.
Given
estrogen
promoting
hormone-receptor-positive
cancers,
has
become
important
molecular
target
for
development
anticancer
agents.
inhibitors
can
be
classified
two
main
groups
based
on
their
chemical
structure:
steroidal
non-steroidal
inhibitors.
This
work
presents
review
literature
from
last
ten
years
regarding
search
new
We
present
directions
search,
taking
account
impact
structure
modifications
activity.
