Polycyclic aromatic compounds,
Год журнала:
2021,
Номер
42(10), С. 7686 - 7696
Опубликована: Ноя. 28, 2021
In
this
research
a
new
derivatives
of
3,3,5-trichloroisatins
and
3,3-dichloroisatins
were
synthesized
in
good
yields
using
catalyst-free
one-pot
reaction
isatins
or
N-alkylisatines,
triphenylphosphine
carbon
tetrachloride
acetonitrile
at
room
temperature.
Because
existing
isatin
core
compounds,
the
antioxidant
activity
was
investigated
2,2-diphenyl-1-picrylhydrazyl
(DPPH)
radical
scavenging
power
compounds
for
reducing
ferric
ion
experiments
comparing
results
with
synthetic
antioxidants
(TBHQ
BHT).
Easy,
simple,
fast
procedure
are
some
advantages
study.
Chemistry & Biodiversity,
Год журнала:
2024,
Номер
21(4)
Опубликована: Фев. 9, 2024
Heterocyclic
compounds
containing
1,2,3-triazole
and
isatin
as
core
structures
have
emerged
promising
drug
candidates
due
to
their
diverse
biological
activities
such
anti-cancer,
antifungal,
antimicrobial,
antitumor,
anti-epileptic,
antiviral,
more.
The
presence
of
1,2,3-triazoles
heterocycles
in
these
hybrids,
both
individually
known
for
medicinal
significance,
has
increasingly
piqued
the
interest
discovery
researchers,
they
seek
delve
deeper
into
extensive
pharmacological
potential
enhancing
therapeutic
efficacy.
Moreover,
hybrid
are
synthetically
accessible
using
readily
available
materials.
Therefore,
there
is
a
pressing
need
provide
comprehensive
overview
existing
knowledge
this
field,
offering
valuable
insights
readers
paving
way
novel
1,2,3-triazole-linked
hybrids
with
potential.
New Journal of Chemistry,
Год журнала:
2022,
Номер
46(6), С. 2863 - 2874
Опубликована: Янв. 1, 2022
A
series
of
isatin
oxime
ether-tethered
aryl
1
H
-1,2,3-triazole
hybrids
were
synthesized
and
screened
for
their
in
vitro
antitubercular
activity
against
the
M.
tuberculosis
H37Rv
strain.
Molecular
hybridization
is
deemed
an
optimistic
approach
in
drug
design
and
the
discovery
of
novel
biologically
active
molecules
as
it
may
advance
their
affinity
potency
while
concurrently
decreasing
associated
resistance
side
effects.
Approximately
20
%
approved
drugs
were
developed
using
this
past
few
years.
Thiazolidinone
one
privileged
pharmacophores
medicinal
chemistry
with
various
biological
activities;
forms
a
functional
unit
several
FDA-approved
drugs.
Consequently,
pharmacophore
has
attracted
attention
many
research
groups
to
further
explore
its
pharmacological
relevance
by
coupling
other
pharmacophoric
moieties.
This
review
presents
concise
account
scholarly
exploits
directed
at
activities
newly
synthesized
thiazolidinone-tagged
molecular
hybrids.
Focused
given
existing
structural
activity
relationship
each
compound
library
toxicity
profile
potent
compounds
including
silico
docking
studies
(where
applicable).
work
would
provide
base
on
which
new
pharmaceuticals
improved
can
be
modelled.
International Journal of Molecular Sciences,
Год журнала:
2025,
Номер
26(5), С. 2144 - 2144
Опубликована: Фев. 27, 2025
Cancer
remains
one
of
the
leading
causes
death
globally,
driving
need
for
effective
therapies.
Targeting
cyclin-dependent
kinase
2
(CDK2),
a
critical
cell
cycle
regulator,
is
promising
approach
cancer
treatment.
This
study
developed
new
group
5-methylisatin
derivatives
with
strong
binding
potential
to
CDK2.
By
combining
isatin
core
various
benzoylhydrazide
substituents,
design
process
was
guided
by
molecular
docking,
dynamic
simulations,
and
ADMET
analysis.
Thirty-one
were
modelled,
subset
synthesised
characterised
their
physicochemical
spectroscopic
properties.
The
analysis
suggested
that
substitutions
at
R2
R3
positions
improved
affinity,
while
modifications
R4
less
favourable.
Hydrogen
bonds
GLU81
LEU83,
along
hydrophobic
interactions,
key
stabilising
complexes.
A
comparison
reference
molecule
(RM)
3-((2,6-Dichlorobenzylidene)hydrazono)indolin-2-one,
showing
inhibitory
activity
similar
doxorubicin,
revealed
several
advantages
derivatives.
multidimensional
comparative
highlighted
significant
improvements
in
active
site
conformational
stability,
fit.
confirmed
comparable
performance
most
areas,
superior
bioavailability
observed
1,
2a,
2b,
3h,
3b,
3e.
These
results
suggest
could
be
CDK2
inhibitors.
Pharmaceutics,
Год журнала:
2025,
Номер
17(4), С. 505 - 505
Опубликована: Апрель 11, 2025
Background/Objectives:
The
isatin
nucleus
is
a
privileged
scaffold
in
drug
discovery,
particularly
due
to
its
proven
relevance
anticancer
research.
Developing
reusable
heterogeneous
3D
catalysts
for
synthesis
represents
critical
challenge
both
industrial
and
academic
contexts.
This
multi
interdisciplinary
work
aimed
design
synthesize
novel
3D-printed
silica-based
porous
catalyst
functionalized
with
palladium,
evaluate
catalytic
performance
synthesis,
assess
the
antiproliferative
activity
of
resulting
compounds
against
tumor
cell
lines
such
as
HeLa,
MCF-7,
MDA-MB231.
Methods:
multifaceted
approach
synthesizing
this
involved
surface
growth
metal–organic
framework
(ZIF-8)
on
silica
support,
followed
by
potassium
silicate
coating
pyrolysis.
Results:
After
detailed
physicochemical
characterization,
was
tested
challenging
“double”
palladium-catalyzed
cross-coupling
reactions
(Suzuki,
Stille,
Heck),
demonstrating
robustness,
reusability,
high
efficiency
producing
bis-1,5-aryl,
alkynyl,
alkenyl-isatin
derivatives.
Importantly,
no
leaching
palladium
species
detected
during
cycles,
further
underscoring
stability
system.
These
isatin-based
exhibited
remarkable
cytotoxicity,
selective
molecules
achieving
nanomolar
potency
MCF-7
cells,
surpassing
reference
drugs
doxorubicin
sunitinib.
Conclusions:
study
not
only
introduces
strategy
fabricating
from
sintered
surfaces
but
also
highlights
new
biomolecules
promising
applications
cancer
