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.
European Journal of Organic Chemistry,
Journal Year:
2023,
Volume and Issue:
27(4)
Published: Dec. 6, 2023
Abstract
Isatin,
also
known
as
indoline‐2,3‐dione,
is
a
fused,
N
‐heterocyclic
aromatic
compound
first
isolated
and
purified
in
1841.
Since
then,
isatin
its
derivatives
emerged
hot
research
topic
for
the
scientific
community.
The
number
of
publications
on
justifies
their
popularity.
Researchers
explored
isatins
potential
candidates
multidisciplinary
areas,
including
medicinal
chemistry,
synthetic
organic
polymer
science.
Synthetic
chemists’
perspective
tailoring
family
members
led
to
more
efficient
synthesis
strategies
which
ring‐opening
reactions
were
particularly
significant
due
product's
importance.
Our
investigation
aims
group
different
types
cascade
ring
expansion
synthesise
fused
heterocyclic
compounds
such
quinolines,
quinazolinones,
acridines,
acridones,
few
spiro
compounds,
all
highlight
an
inevitable
role
field
chemistry.
The Journal of Organic Chemistry,
Journal Year:
2023,
Volume and Issue:
88(19), P. 14216 - 14221
Published: Sept. 7, 2023
An
efficient
five-component
condensation
reaction
of
isatin,
malononitrile,
secondary
amines,
alcohols,
and
molecular
oxygen
was
discovered.
The
performed
in
a
one-pot
fashion,
it
does
not
require
any
metal
catalyst.
It
gives
straightforward
access
to
structurally
diverse
2-oxo-3-aminoindoline-3-carboxylates
moderate
yields
(70-88%).
scope
the
successfully
demonstrated
by
synthesizing
series
3-functionalized
2-oxindoles
varying
amine,
alcohol
components.
Advanced Synthesis & Catalysis,
Journal Year:
2023,
Volume and Issue:
366(2), P. 316 - 322
Published: Dec. 18, 2023
Abstract
A
domino
S
N
Ar‐
ih
DA/
r
DA
reaction
was
developed
from
rarely
exploited
3‐fluoro‐1,2,4‐triazines
with
bifunctional
alkyne
tethered
nucleophiles
to
construct
various
fused
non‐aromatic/heteroaromatic
bicycles
in
yields
ranging
56
99%,
notably
within
the
family
of
valuable
spirooxindole
derivatives.
In
this
study,
challenging
enantioselective
phase‐transfer
catalyzed
arylation
a
sulfonyl‐triazine
also
demonstrated
up
66%
ee.
both
racemic
and
asymmetric
processes,
nature
leaving
group
at
C3
key
successfully
achieve
these
sequences.
