ChemistrySelect,
Journal Year:
2024,
Volume and Issue:
9(46)
Published: Dec. 1, 2024
Abstract
We
synthesized
a
novel
compound
library
featuring
spirooxindole
core
structure
combined
with
various
heterocycles,
including
benzofuran,
benzothiophene,
and
thiophene
scaffolds.
Evaluation
using
MTT
assays
against
HepG2,
4T1,
MDA‐MB‐231
cells
revealed
the
most
potent
candidate,
hybrid
5c
,
an
IC50
of
5
±
0.6
µM
inducing
G2/M
phase
cell
cycle
arrest,
inhibition
wound
healing,
induction
ROS.
Selected
conjugates
exhibited
significant
inhibitory
potential
MDM2,
KD
values
ranging
from
0.0531
to
16.8
µM.
Notably,
salt
analogue
5q
demonstrated
highest
activity
at
K
D
=
53.1
nM.
Molecular
docking
studies
excellent
accommodation
designed
compounds
within
MDM2
receptor.
All
displayed
favorable
ADME
profiles,
suggesting
their
as
lead
for
further
optimization.
RSC Advances,
Journal Year:
2024,
Volume and Issue:
14(8), P. 5547 - 5565
Published: Jan. 1, 2024
Spiro
heterocycle
frameworks
are
a
class
of
organic
compounds
that
possesses
unique
structural
features
making
them
highly
sought-after
targets
in
drug
discovery
due
to
their
diverse
biological
and
pharmacological
activities.
Future Medicinal Chemistry,
Journal Year:
2025,
Volume and Issue:
unknown, P. 1 - 19
Published: March 19, 2025
TB
drug
discovery
needs
scientists'
attention
since
resistance
in
TB,
including
extensively
drug-resistant
(XDR-TB)
and
multidrug-resistant
(MDR-TB),
is
a
major
healthcare
concern.
Since
millions
of
fatalities
from
tuberculosis
are
recorded
each
year,
there
an
urgent
need
to
discover
new
anti-tubercular
medications
that
will
either
eradicate
or
control
the
disease.
Spiro
compounds
have
garnered
lot
medicinal
chemistry
these
days
because
various
biological
activities
mainly
their
adaptability
structural
resemblance
significant
pharmacophores.
This
article
overviews
synthesis
activity
spirocyclic
as
agents.
Both
synthesized
naturally
occurring
spiro
chemicals
exhibit
antitubercular
properties.
The
promising
potential
shown
by
some
has
attracted
scientists
explore
them
further
develop
molecules
with
improved
pharmacodynamic
pharmacokinetic
properties
mechanisms
action
enhanced
safety
efficacy
tuberculosis.
current
review
covers
exploration
year
2004
2024
for
combat
Tuberculosis.
gives
comprehensive
advancements
this
scaffold
which
would
help
logical
design
powerful,
less
toxic,
more
effective
anti-TB
molecules.
Green Synthesis and Catalysis,
Journal Year:
2023,
Volume and Issue:
5(1), P. 1 - 13
Published: Aug. 15, 2023
Spirooxindole
is
a
compound
with
unique
framework
and
broad
bioactivities
in
medicine.
In
this
study,
we
have
reviewed
various
approaches
or
methods
synthesizing
spirooxindole
derivatives
focused
on
green
synthesis.
Synthesis
of
spirooxindoles
mainly
carried
out
through
multicomponent
reactions
combined
such
as
the
use
heterogeneous
catalysts
(nano-sized,
magnetic,
metal-complex,
metal-organic
catalysts),
deep
eutectic
solvent,
solvent-free
reactions,
catalyst-free
well
ultrasonic
microwaves
irradiation.
The
method
addition
to
obtaining
high
yields,
it
also
offers
reductions
hazardous
chemicals,
energy
use,
purification
processes,
waste
generation.
As
result,
synthesis
are
more
environmentally
friendly.
Applied Organometallic Chemistry,
Journal Year:
2024,
Volume and Issue:
38(4)
Published: Feb. 7, 2024
A
highly
efficient,
green,
and
multicomponent
reaction
method
has
been
developed
for
the
diversity‐oriented
synthesis
of
32
spirooxindole
derivatives
via
formation
cascade
C–N,
C–O,
C–S
bonds.
The
involved
starch‐capped
zinc
oxide
nanocomposite
as
an
effective
heterogeneous
catalyst
with
synergistic
application
ultrasound
on‐water
synthesis.
By
employing
this
approach,
all
desired
products
were
successfully
obtained
high
yields
comparatively
short
times.
Furthermore,
employed
in
process
exhibited
excellent
recyclability,
allowing
its
recovery
reuse
up
to
eight
consecutive
runs
without
any
loss
catalytic
activity.
greenness
protocol
was
evaluated
by
various
green
metrics
such
E‐factor
eco‐score,
result
showed
acceptability
present
organic
ChemistrySelect,
Journal Year:
2023,
Volume and Issue:
8(11)
Published: March 14, 2023
Abstract
Herein,
we
present
a
one‐pot,
three‐component
synthesis
of
spirooxindole‐oxofuran
carboxylate
derivatives
(
4
–
d
)
through
the
Huisgen
reaction.
The
newly
synthesized
spirocyclic
compounds
were
tested
for
in
vitro
antiproliferative
efficacy
against
60
human
cancer
cell
lines
at
National
Cancer
Institute
(NCI)
United
States.
screening
results
indicated
that
two
spirooxindole
compounds,
b
and
c
,
possessed
strongest
anti‐cancer
terms
percentage
growth
inhibition
(%
GI),
with
values
34.17
38.19
10
−5
M
concentration
CNS
panel‘s
SNB‐75
line,
respectively.
Furthermore,
molecular
docking
investigations
demonstrated
binding
affinity
P2Y12
receptor.
compound
which
exhibited
strong
activity
high
energies
might
therefore,
serve
as
potential
lead
molecule
development
more
effective
agents.
International Journal of Molecular Sciences,
Journal Year:
2023,
Volume and Issue:
24(8), P. 7336 - 7336
Published: April 15, 2023
A
highly
stereo-selective,
one-pot,
multicomponent
method
was
chosen
to
synthesize
the
novel
functionalized
1,
3-cycloaddition
spirooxindoles
(SOXs)
(4a-4h).
Synthesized
SOXs
were
analyzed
for
their
drug-likeness
and
ADME
parameters
screened
anticancer
activity.
Our
molecular
docking
analysis
revealed
that
among
all
derivatives
of
(4a-4h),
4a
has
a
substantial
binding
affinity
(∆G)
-6.65,
-6.55,
-8.73,
-7.27
Kcal/mol
with
CD-44,
EGFR,
AKR1D1,
HER-2,
respectively.
functional
study
demonstrated
SOX
impact
on
human
cancer
cell
phenotypes
exhibiting
abnormality
in
cytoplasmic
nuclear
architecture
as
well
granule
formation
leading
death.
treatment
robustly
induced
reactive
oxygen
species
(ROS)
generation
cells
observed
by
enhanced
DCFH-DA
signals.
Overall,
our
results
suggest
(4a)
targets
HER-2
induces
ROS
cells.
We
conclude
could
be
explored
potential
chemotherapeutic
molecule
against
various
cancers
appropriate
pre-clinical
vitro
vivo
model
systems.
