Anticancer and anti-inflammatory effects of novel ethyl pyrazole derivatives having sulfonamide terminal moiety
Bioorganic Chemistry,
Год журнала:
2024,
Номер
153, С. 107825 - 107825
Опубликована: Сен. 16, 2024
Язык: Английский
Transition metal complexes of sulfonamide-based Schiff base ligand: Synthesis, Characterization, A Biological assessment, DFT, and ADME studies
Journal of Molecular Structure,
Год журнала:
2024,
Номер
unknown, С. 140907 - 140907
Опубликована: Ноя. 1, 2024
Язык: Английский
Multifaceted Sulfonamide-Derived Thiosemicarbazones: Combining Metal Chelation and Carbonic Anhydrases Inhibition in Anticancer Therapy
International Journal of Molecular Sciences,
Год журнала:
2025,
Номер
26(3), С. 1225 - 1225
Опубликована: Янв. 30, 2025
The
selective
inhibition
of
key
enzymes,
such
as
carbonic
anhydrases
(CAs
IX
and
XII),
which
are
overexpressed
in
cancer
tissues,
has
emerged
a
promising
strategy
research.
However,
multitarget
approach
is
often
preferred
to
achieve
enhanced
therapeutic
outcomes.
In
this
study,
aryl
sulfonamides
were
conjugated
with
thiosemicarbazone
moiety
enable
dual
functionality:
the
CAs
chelation
metal
cations.
Several
structural
factors
systematically
modified,
including
position
sulfonamido
group,
length
linker,
nature
aromatic
residue,
type
substituents.
Tumor-associated
XII
was
evaluated
using
stopped-flow
CO2
hydrase
assay,
constants
(Ki)
determined.
most
compounds
further
analyzed
through
molecular
docking
simulations.
Metal
capabilities
UV–Vis
spectroscopy,
while
antiproliferative
activities
measured
sulforhodamine
B
(SBR)
assay.
Additionally,
holotomographic
3D
microscopy
employed
investigate
mechanisms
cell
death.
Sulfonamido-derived
Schiff
bases
synthesized
three-step
procedure
that
did
not
require
column
chromatography
purification:
(1)
isothiocyanation
amino-sulfonamides,
(2)
nucleophilic
addition
hydrazine,
(3)
acid-promoted
condensation
different
aldehydes
(benzaldehydes
or
pyridine-2-carboxaldehyde).
exhibited
low
nanomolar
submicromolar
range,
selectivity
largely
influenced
by
features.
Notably,
m-sulfonamide
derivative
5b,
bearing
pyridin-2-yl
demonstrated
potent
CA
(Ki
=
4.9
nM)
5.6
nM).
it
efficiently
chelated
Fe2+,
Fe3+,
Cu2+
showed
activity
(GI50
4.5–10
µM).
Mechanistic
studies
revealed
apoptosis
involved
its
mode
action.
Therefore,
synergistic
integration
thiosemicarbazones
represents
an
effective
for
development
multimodal
anticancer
agents.
Язык: Английский
Development of novel amino-benzenesulfonamide derivatives and their analogues as carbonic anhydrase inhibitors: Design, synthesis, anticancer activity assessment, and pharmacokinetic studies using UPLC-MS/MS
Bioorganic Chemistry,
Год журнала:
2025,
Номер
159, С. 108335 - 108335
Опубликована: Март 6, 2025
Язык: Английский
Mechanochemical syntheses of N-acyl sulfinamidines via iron-nitrenoids and their conversions to sulfur(VI) derivatives
Green Synthesis and Catalysis,
Год журнала:
2025,
Номер
unknown
Опубликована: Апрель 1, 2025
Язык: Английский
Synthesis of S-alkylated oxadiazole bearing imidazo[2,1-b]thiazole derivatives targeting breast cancer: In vitro cytotoxic evaluation and in vivo radioactive tracing studies
Bioorganic Chemistry,
Год журнала:
2024,
Номер
153, С. 107935 - 107935
Опубликована: Ноя. 2, 2024
Язык: Английский
Molecular docking, microwave-assisted synthesis, characterization, and preliminary evaluation of the anti-microbial activity of new sulfonamide derivatives of the 1, 2, 4-triazole-3-thiol ring system
Ali. Abdulhadi. Mosleh,
Zainab Abdelhadi Dakhel
Pharmacia,
Год журнала:
2024,
Номер
71, С. 1 - 9
Опубликована: Сен. 3, 2024
A
new
sulfonamide
derivative
containing
a
1,2,4-Triazole-3-thiol
ring
was
synthesized
and
characterized
using
FT-IR
1
H-NMR.
The
microwave-assisted
chemical
synthesis
of
the
system
resulted
in
good
yield
purity.
synthetic
compounds
were
then
subjected
to
vitro
evaluation
for
antimicrobial
study.
All
show
high
activity
against
Gram-positive
bacteria
(
S.
aureus
,
pneumonia
B.
subtilis
)
Gram-negative
P.
aeruginosa
H.
pylori
),
with
less
N.
gonorrhoeae
E.
coli
).
Also,
it
shows
fungi
C.
albicans
In
this
study,
we
utilized
computational
methods
design
derivatives
that
target
carbonic
anhydrase
enzyme
(PDB:
4YGF).
interact
enzyme’s
active
site,
resulting
disturbance
acid-base
balance
affecting
virulence
pathogenicity.
Язык: Английский