RSC Advances,
Journal Year:
2024,
Volume and Issue:
14(9), P. 5690 - 5728
Published: Jan. 1, 2024
VEGF,
an
important
category
of
tyrosine
kinases,
and
its
receptors
(VEGFR)
are
hyper-activated
in
different
cancers.
The
recently
reported
indolyl
analogs
with
potential
antineoplastic
VEGFR
inhibitory
properties
highlighted.
Molecules,
Journal Year:
2023,
Volume and Issue:
28(18), P. 6603 - 6603
Published: Sept. 13, 2023
The
COVID-19
pandemic
has
posed
a
significant
threat
to
society
in
recent
times,
endangering
human
health,
life,
and
economic
well-being.
disease
quickly
spreads
due
the
highly
infectious
SARS-CoV-2
virus,
which
undergone
numerous
mutations.
Despite
intense
research
efforts
by
scientific
community
since
its
emergence
2019,
no
effective
therapeutics
have
been
discovered
yet.
While
some
repurposed
drugs
used
control
global
outbreak
save
lives,
none
proven
universally
effective,
particularly
for
severely
infected
patients.
Although
spread
of
is
generally
under
control,
anti-SARS-CoV-2
agents
are
still
needed
combat
current
future
infections.
This
study
reviews
most
promising
containing
indolyl
heterocycle,
an
essential
scaffold
many
alkaloids
with
diverse
bio-properties
various
biological
fields.
also
discusses
natural
synthetic
indole-containing
compounds
properties
computer-aided
drug
design
(in
silico
studies)
optimizing
hits/leads.
Organic & Biomolecular Chemistry,
Journal Year:
2024,
Volume and Issue:
22(8), P. 1727 - 1732
Published: Jan. 1, 2024
In
this
study,
we
developed
a
novel
methodology
involving
base-controlled,
rongalite-mediated
reductive/aldol
reaction,
followed
by
cyclization
of
isatylidene
malononitriles/cyanoacetates,
resulting
in
the
synthesis
spiro[2,3-dihydrofuran-3,3'-oxindole].
Additionally,
have
disclosed
dimerization
process
for
malononitriles,
yielding
dispiro[cyclopent-3'-ene]bisoxindole.
The
utilization
rongalite
reaction
serves
dual
purpose,
acting
both
as
reducing
agent
and
C1
synthon.
approach
has
several
advantages
like
simple
setup,
wide
substrate
scope,
requiring
less
time,
using
water
green
solvent,
no
metal
or
catalyst
is
required
products
can
be
easily
isolated
Chemistry,
Journal Year:
2025,
Volume and Issue:
7(1), P. 18 - 18
Published: Feb. 1, 2025
Spirooxindoles
are
a
family
of
heterocyclic
compounds
which
bear
the
oxindole
nucleus
in
their
structures,
have
considerable
pharmaceutical
potential
and
been
linked
to
various
drugs
for
treatment
diverse
diseases.
In
this
work,
wide
variety
spirooxindoles
bearing
pyrrolizinic
were
obtained
by
1,3-dipolar
cycloaddition
reaction
between
substituted
isatins,
trans-3-benzoyl
acrylic
acid
L-proline.
approach,
target
products
9a–m
40–86%
yields
under
heating
reflux
methanol
over
2
h.
Similarly,
containing
an
indolizinic
11a–j
45–69%
switching
L-proline
pipecolic
acetonitrile
8
The
antibacterial
activity
was
evaluated
against
P.
aeruginosa,
K.
pneumoniae,
E.
coli,
S.
aureus,
N.
gonorrhoeae,
also
including
inverse
docking
analysis.
Results
show
that
9f
11i,
most
active
while
9d
9m
displayed
higher
gonorrhoeae.
Inverse
analysis
showed
9b,
11a
11e,
11i
high
affinity
protein
6TYM
7Q6S,
involved
biological
pathways
cancer
Parkinson
ChemistrySelect,
Journal Year:
2025,
Volume and Issue:
10(6)
Published: Feb. 1, 2025
Abstract
In
this
study,
we
develop
a
novel
methodology
involving
rongalite‐mediated
domino
reductive/aldol
reaction,
followed
by
spiro‐lactonization
of
2‐oxoindolin‐3‐ylidene
acetates/malonates
in
presence
base
to
synthesis
3,3′‐spirooxindole
γ
‐butyrolactone.
The
detail
such
as
effect
solvent,
different
and
substrate
has
been
carried
out.
Scale
up
is
also
done.
Sodium
hydroxymethanesulfinate
dihydrate
(rongalite)
concurrently
dual
role
context;
it
acts
reducing
agent
well
C1
synthon.
This
approach
offers
several
advantages,
being
metal‐
catalyst‐free,
simple
reaction
protocol,
having
wide
scope,
using
water
green
providing
good
excellent
yields
the
products
under
mild
conditions.
Pharmaceuticals,
Journal Year:
2025,
Volume and Issue:
18(2), P. 274 - 274
Published: Feb. 19, 2025
The
p53,
often
referred
to
as
the
"guardian
of
genome",
is
a
well-established
tumor-suppressor
protein
that
plays
critical
role
in
regulating
cell
cycle,
DNA
repair,
differentiation,
and
apoptosis,
with
its
activity
primarily
modulated
by
MDM2
(murine
double
minute
2,
also
known
HDM2
humans).
Disrupting
protein-protein
interaction
between
p53
represents
promising
therapeutic
strategy
for
developing
anticancer
agents.
Recent
studies
have
shown
several
spirooxindole-containing
compounds
exhibit
significant
antitumor
properties,
inhibiting
p53-MDM2
interaction.
This
review
provides
an
overview
structure-based
spirooxindoles
could
potential.
It
highlights
findings
from
past
decade
concerning
their
antiproliferative
properties
implications
interfering
discussion
includes
various
analogs
candidates
optimizing
leads
drug
discovery
programs
aimed
at
novel
clinically
effective
