Journal of Enzyme Inhibition and Medicinal Chemistry,
Год журнала:
2021,
Номер
36(1), С. 987 - 999
Опубликована: Янв. 1, 2021
As
one
of
the
most
lethal
malignancies,
lung
cancer
is
considered
to
account
for
approximately
one-fifth
all
malignant
tumours-related
deaths
worldwide.
This
study
reports
synthesis
and
in
vitro
biological
assessment
two
sets
3-methylbenzofurans
(4a–d,
6a–c,
8a–c
11)
3-(morpholinomethyl)benzofurans
(15a–c,
16a–b,
17a–b
18)
as
potential
anticancer
agents
towards
non-small
cell
carcinoma
A549
NCI-H23
lines,
with
VEGFR-2
inhibitory
activity.
The
target
benzofuran-based
derivatives
efficiently
inhibited
growth
both
lines
IC50
spanning
ranges
1.48–47.02
0.49–68.9
µM,
respectively.
three
active
benzofurans
(4b,
15a
16a)
were
further
investigated
their
effects
on
cycle
progression
apoptosis
(for
4b)
lines.
Furthermore,
4b,
16a
displayed
good
activity
equal
77.97,
132.5
45.4
nM,
Journal of Enzyme Inhibition and Medicinal Chemistry,
Год журнала:
2018,
Номер
33(1), С. 1095 - 1107
Опубликована: Янв. 1, 2018
Herein,
we
report
the
synthesis
of
different
novel
sets
coumarin-6-sulfonamide
derivatives
bearing
functionalities
(4a,
b,
8a–d,
11a–d,
13a,
and
15a–c),
in
vitro
evaluation
their
growth
inhibitory
activity
towards
proliferation
three
cancer
cell
lines;
HepG2
(hepatocellular
carcinoma),
MCF-7
(breast
cancer),
Caco-2
(colon
cancer).
cells
were
most
sensitive
to
influence
target
coumarins.
Compounds
13a
15a
emerged
as
active
members
against
(IC50
=
3.48
±
0.28
5.03
0.39
µM,
respectively).
able
induce
apoptosis
cells,
assured
by
upregulation
Bax
downregulation
Bcl-2,
besides
boosting
caspase-3
levels.
Besides,
compound
induced
a
significant
increase
percentage
at
Pre-G1
6.4-folds,
with
concurrent
arrest
G2-M
phase
5.4-folds
compared
control.
Also,
displayed
annexin
V-FITC
positive
apoptotic
from
1.75–13.76%.
Moreover,
QSAR
models
established
explore
structural
requirements
controlling
anti-proliferative
activities.
Journal of Enzyme Inhibition and Medicinal Chemistry,
Год журнала:
2019,
Номер
34(1), С. 322 - 332
Опубликована: Янв. 1, 2019
In
connection
with
our
research
program
on
the
development
of
novel
anticancer
candidates,
herein
we
report
design
and
synthesis
series
1-(2-methyl-6-arylpyridin-3-yl)-3-phenylureas
5a–l.
The
target
pyridins
were
evaluated
for
their
in
vitro
activity
against
two
cancer
cell
lines:
non-small
lung
A549
line
colon
HCT-116
line.
Compound
5l
emerged
as
most
active
congener
towards
both
lines
IC50
values
equal
to
3.22
±
0.2
2.71
0.16
µM,
respectively,
which
are
comparable
those
Doxorubicin;
2.93
0.28
3.10
0.22,
respectively.
Furthermore,
compound
stood
out
potent
pyridine
derivative
(mean
%
GI
=
40),
at
US-NCI
Developmental
Therapeutic
Program
assay,
broad-spectrum
antitumor
tested
from
all
subpanels.
was
able
provoke
apoptosis
cells
evidenced
by
decreased
expression
anti-apoptotic
Bcl-2
protein,
enhanced
pro-apoptotic
proteins
levels;
Bax,
cytochrome
C,
p53,
caspase-3
caspase-9.
Moreover,
disrupted
cycle
via
alteration
Sub-G1
phase
arresting
G2-M
stage.
Also,
showed
a
significant
increase
percent
annexinV-FITC
positive
apoptotic
1.99
15.76%.
Journal of Saudi Chemical Society,
Год журнала:
2021,
Номер
25(8), С. 101284 - 101284
Опубликована: Июнь 19, 2021
Chemotherapy
is
an
important
therapeutic
approach
for
the
treatment
of
cancer.
Currently,
many
anticancer
drugs
are
available
in
market
that
plays
role
cancer
treatment,
but
concerns
such
as,
drug
resistance
and
side
effects
create
urgent
need
development
new
anti-tumor
with
high
potency
less
effects.
Heterocycles
great
interest
due
to
their
fascinating
activity.
Among
them,
1,3,4-oxadiazoles
showed
attracting
activity
its
derivatives
under
clinical
trials
Hybridization
1,3,4-oxadiazole
moiety
other
heterocyclic
pharmacophoresis
a
promising
overcome
various
disadvantages
current
as
resistance,
toxicity,
Thus,
1,3,4-oxadiazole-heterocycle
hybrids
occupy
significant
position
discovery
drugs.
reported
oxadiazole-based
reviewed
here,
compounds
45i,
59j,
62x
highest
IC50
values
nanomolar
range.
This
review
summarizes
recent
developments
potential,
structure–activity
relationships,
mechanisms
actions
hybrids.
Molecules,
Год журнала:
2018,
Номер
23(6), С. 1459 - 1459
Опубликована: Июнь 15, 2018
In
our
endeavor
towards
the
development
of
effective
anticancer
agents,
a
novel
series
pyridine-ureas
8a–n
were
synthesized.
All
newly
prepared
derivatives
evaluated
in
vitro
for
their
growth
inhibitory
activity
proliferation
breast
cancer
MCF-7
cell
line.
Compounds
8e
and
8n
found
to
be
most
active
congeners
against
cells
(IC50
=
0.22
1.88
µM
after
48
h
treatment;
0.11
0.80
72
treatment,
respectively)
with
increased
compared
reference
drug
doxorubicin
1.93
µM).
Moreover,
eight
selected
pyridines
8b,
8d,
8e,
8i,
8j
8l–n
according
US-NCI
protocol.
Pyridines
8b
proved
agents
NCI
assay
mean
inhibition
43
49%,
respectively.
Both
exhibited
anti-proliferative
all
tested
lines
from
subpanels
(GI
8b;
12–78%,
GI
8e;
15–91%).
screened
VEGFR-2.
compounds
inhibited
VEGFR-2
at
micromolar
IC50
values
5.0
±
1.91
3.93
0.73
µM,
The
filtered
Lipinski
Veber
rules
them
passed
these
filters.
Finally,
several
ADME
descriptors
predicted
through
theoretical
kinetic
study.
