Archiv der Pharmazie,
Год журнала:
2020,
Номер
353(3)
Опубликована: Янв. 21, 2020
Abstract
The
isatin
framework
is
a
useful
template
for
the
development
of
novel
anticancer
agents.
This
exemplified
by
fact
that
several
isatin‐based
agents,
such
as
semaxanib,
sunitinib,
nintedanib,
and
hesperadin,
are
already
in
use
or
under
clinical
trials
treatment
diverse
kinds
cancers.
Isatin‐based
hybrids
could
be
obtained
incorporating
other
pharmacophores
into
skeleton
they
have
potential
to
overcome
drug
resistance
with
reduced
side
effects.
Thus,
may
provide
attractive
scaffolds
review
covers
recent
advances
activity,
covering
articles
published
between
2001
2019.
activities
these
molecules
structure–activity
relationships
also
discussed.
purpose
this
article
set
up
direction
design
high
efficacy
low
toxicity.
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%.
Pharmaceuticals,
Год журнала:
2022,
Номер
15(5), С. 536 - 536
Опубликована: Апрель 27, 2022
Isatin,
chemically
an
indole-1H-2,3-dione,
is
recognised
as
one
of
the
most
attractive
therapeutic
fragments
in
drug
design
and
development.
The
template
has
turned
out
to
be
exceptionally
useful
for
developing
new
anticancer
scaffolds,
evidenced
by
increasing
number
isatin-based
molecules
which
are
either
clinical
use
or
trials.
Apart
from
its
promising
antiproliferative
properties,
isatin
shown
potential
treating
Neglected
Tropical
Diseases
(NTDs)
not
only
a
parent
core,
but
also
attenuating
activities
various
pharmacophores.
objective
this
mini-review
keep
readers
up
date
on
latest
developments
biological
targeting
cancer
NTDs
such
tuberculosis,
malaria,
microbial
infections.
Journal of Enzyme Inhibition and Medicinal Chemistry,
Год журнала:
2023,
Номер
38(1)
Опубликована: Апрель 25, 2023
In
this
work,
new
isatin-based
sulphonamides
(6a-i,
11a-c,
12a-c)
were
designed
and
synthesised
as
potential
dual
VEGFR-2
carbonic
anhydrase
inhibitors
with
anticancer
activities.
Firstly,
all
target
isatins
examined
for
in
vitro
antitumor
action
on
NCI-USA
panel
(58
tumour
cell
lines).
Then,
the
most
potent
derivatives
CA
inhibitory
towards
physiologically
relevant
hCA
isoforms
I,
II,
tumour-linked
IX
isoform,
addition,
activity
was
evaluated.
The
failed
to
inhibit
that
could
be
attributable
steric
effect
of
neighbouring
methoxy
group,
whereas
they
displayed
effect.
Following
that,
11b
12b
tested
their
influence
cycle
disturbance,
apoptotic
potential.
Finally,
detailed
molecular
modelling
analyses,
including
docking
dynamics,
carried
out
assess
binding
mode
stability
isatins.
