Results in Chemistry,
Год журнала:
2024,
Номер
7, С. 101476 - 101476
Опубликована: Янв. 1, 2024
The
present
study
reports
the
synthesis
of
sulphonamide-azaheterocycle
conjugates
(3
a-j)
and
evaluates
its
in
vitro
anticancer
activity
against
breast
cancer
cell
line
(MCF-7)
liver
(HepG2).
compound
3g
was
found
to
be
most
active
with
IC50
values
40.54
±
0.25
μg/ml
MCF
7
55.38
0.18
HepG2
line.
3h
value
36.70
0.90
54.75
0.68
as
compared
standard
drug
5-fluorouracil
(26.08
0.82
45.50
2.35
μg/ml).
compounds
3
a-j
showed
characteristic
changes,
particularly
nucleus,
which
were
observed
through
nuclear
staining
fluorescent
dye
DAPI.
has
shown
strong
anti-inflammatory
31.17
0.23
μg/ml.
Furthermore,
anti-diabetic
exhibited
significant
34.51
1.31
33.87
1.54
acarbose.
Compounds
3a,
3b,
3d,
3f,
displayed
a
antiangiogenic
effect,
an
score
1.34,
1.28,
1.32,
1.41,
1.41
1.45.
Moreover,
silico
bioactivity
prediction
studies
demonstrated
interactions
between
putative
targets.
Results
DFT
analysis
highlighted
that
possesses
favorable
electronic
structure
possibility
having
promising
potential
biological
applications.
binding
affinities
docking
among
all
tested
both
HER2
(PDB:
3PP0)
EGFR
4HJO).
Expert Opinion on Drug Discovery,
Год журнала:
2022,
Номер
17(5), С. 501 - 512
Опубликована: Фев. 23, 2022
Sulfur-containing
functional
groups
are
privileged
motifs
that
occur
in
various
pharmacologically
effective
substances
and
several
natural
products.
Various
functionalities
found
with
a
sulfur
atom
at
diverse
oxidation
states,
as
illustrated
by
thioether,
sulfoxide,
sulfone,
sulfonamide,
sulfamate,
sulfamide
functions.
They
valuable
scaffolds
the
field
of
medicinal
chemistry
part
large
array
approved
drugs
clinical
candidates.Herein,
authors
review
current
research
on
development
organosulfur-based
drug
discovery.
This
article
also
covers
details
their
roles
new
lead
compounds
reported
literature
over
past
five
years
2017-2021.Given
its
prominent
role
importance
discovery,
has
attracted
continuing
interest
been
used
design
demonstrate
variety
biological
pharmacological
feature
activities.
Overall,
sulfur's
continues
to
grow.
However,
many
remain
underused
small-molecule
discovery
deserve
special
attention
armamentarium
for
treating
diseases.
Research
efforts
still
required
synthetic
methodology
direct
access
these
functions
late-stage
functionalization.
Pharmaceutics,
Год журнала:
2023,
Номер
15(5), С. 1348 - 1348
Опубликована: Апрель 27, 2023
The
electron-rich
five-membered
aromatic
aza-heterocyclic
imidazole,
which
contains
two
nitrogen
atoms,
is
an
important
functional
fragment
widely
present
in
a
large
number
of
biomolecules
and
medicinal
drugs;
its
unique
structure
beneficial
to
easily
bind
with
various
inorganic
or
organic
ions
molecules
through
noncovalent
interactions
form
variety
supramolecular
complexes
broad
potential,
being
paid
increasing
amount
attention
regarding
more
contributions
imidazole-based
for
possible
application.
This
work
gives
systematical
comprehensive
insights
into
research
on
complexes,
including
anticancer,
antibacterial,
antifungal,
antiparasitic,
antidiabetic,
antihypertensive,
anti-inflammatory
aspects
as
well
ion
receptors,
imaging
agents,
pathologic
probes.
new
trend
the
foreseeable
near
future
toward
chemistry
also
prospected.
It
hoped
that
this
provides
help
rational
design
drug
agents
effective
diagnostic
pathological
RSC Advances,
Год журнала:
2025,
Номер
15(5), С. 3928 - 3953
Опубликована: Янв. 1, 2025
This
review
studies
magnetically
recoverable
catalysts
designed
for
the
efficient
multicomponent
synthesis
of
organosulfur
compounds.
These
enhance
process
by
combining
efficiency
with
environmental
sustainability.
Molecules,
Год журнала:
2022,
Номер
27(3), С. 671 - 671
Опубликована: Янв. 20, 2022
Since
the
synthesis
of
prontosil
first
prodrug
shares
their
chemical
moiety,
sulfonamides
exhibit
diverse
modes
actions
to
serve
as
antimicrobials,
diuretics,
antidiabetics,
and
other
clinical
applications.
This
inspiring
nucleus
has
promoted
several
research
groups
investigate
new
members
exploring
In
this
study,
a
novel
series
5(4H)-oxazolone-based-sulfonamides
(OBS)
9a–k
were
synthesized,
antibacterial
antifungal
activities
evaluated
against
wide
range
Gram-positive
-negative
bacteria
fungi.
Most
tested
compounds
exhibited
promising
activity
both
particularly
OBS
9b
9f.
Meanwhile,
compound
9h
showed
most
potent
activity.
Moreover,
9a,
9b,
9f
that
inhibited
bacterial
growth
at
lowest
concentrations
subjected
further
evaluation
for
anti-virulence
Pseudomonas
aeruginosa
Staphylococcus
aureus.
Interestingly,
three
reduced
biofilm
formation
diminished
production
virulence
factors
in
P.
S.
Bacteria
use
signaling
system,
quorum
sensing
(QS),
regulate
virulence.
context,
silico
study
been
conducted
assess
ability
compete
with
QS
receptors.
The
marked
bind
hinder
receptors,
indicating
could
be
due
blocking
QS,
system
controls
Furthermore,
anticancer
performed
such
derivatives.
variable
anti-tumor
activities,
specifically
9k,
different
cancer
lines.
Conclusively,
can
agents.
Arabian Journal of Chemistry,
Год журнала:
2023,
Номер
16(8), С. 104916 - 104916
Опубликована: Апрель 17, 2023
The
ligands,
4-(2-Hydroxy-naphthalen-1-ylazo)-N-thiazol-2-yl-benzenesulfonamide
(H2TNBS)
and
N-(3,4-Dimethyl-isoxazol-5-yl)-4-(2-hydroxy-naphthalen-1-ylazo)-benzenesulfonamide
(H2INBS),
synthesized
in
the
current
investigation
have
been
characterized
used
for
synthesizing
divalent
copper
complexes
by
their
reaction
with
a
number
of
Cu(II)
salts.
Spectral
analytical
methods
applied
structures'
investigation.
Morphology
compounds
investigated
using
TEM
technique
which
joint
results
X-ray
powder
diffraction
spectroscopy
confirmed
precipitation
both
ligands
nanometric
scale.
Formation
1:1
or
2:1
(M:L)
ratio
was
asserted
results.
Ultraviolet–visible
spectra
magnetic
moment
were
to
demonstrate
geometry
around
Cu
centers
be
4
coordinated
square
planar.
under
interest
screened
against
selected
microorganisms
including
Gram-positive
Gram-negative
bacteria,
unicellular
multicellular
fungus
showing,
most
compounds,
enhancement
activity
upon
chelation.
cell
lines
A-549
(human
lung
cancer
line)
Panc-1
pancreatic
chosen
check
antitumor
efficiency
compounds;
Vinblastine
as
standard.
Finally,
chelates
toward
mimicking
protein
phenoxazinone
synthase
o-
aminophenol
(OAP)
substrate
DMF
is
solvent.
presented
extremely
high
chloro
complex
nitro
6
TOF
numbers
from
390.48
467.01
h−1,
respectively.
least
afforded
acetato
2
5.
Molecular Diversity,
Год журнала:
2024,
Номер
unknown
Опубликована: Июнь 4, 2024
Abstract
The
emergence
of
diverse
infections
worldwide,
which
is
a
serious
global
threat
to
human
existence,
necessitates
the
urgent
development
novel
therapeutic
candidates
that
can
combat
these
diseases
with
efficacy.
Molecular
hybridization
has
been
established
as
an
efficient
technique
in
designing
bioactive
molecules
capable
fighting
infections.
Isatin,
core
nucleus
array
compounds
biological
properties
be
modified
at
different
positions
leading
creation
drug
targets,
active
area
medicinal
chemistry.
This
review
containing
published
articles
from
2005
2022
highlights
isatin
hybrids
have
synthesized
and
reported
literature
alongside
discussion
on
their
properties.
enriched
structure–activity
relationship
studies
discussed
provides
insights
for
rational
design
tailored
effective
inspired
by
nature.
