Arabian Journal of Chemistry,
Journal Year:
2023,
Volume and Issue:
16(8), P. 104956 - 104956
Published: May 3, 2023
New
thiadiazole
sulfonamide
derivatives
were
designed
as
human
carbonic
anhydrase
inhibitors
(hCAIs)
to
develop
robust
and
novel
anticancer
agents.
Tail
modification
approach
was
considered
in
designing
the
target
compounds
which
synthesized
following
two-step
procedure
starting
from
5-acetyl-3-N-(4-sulfamoylphenyl)-2-imino-1,3,4-thiadiazoline.
Cytotoxic
evaluation
revealed
potent
diazene
derivative
2
with
IC50
1.18
μM,
5.28
μM
7.15
against
MCF-7,
Caco2
HepG-2,
respectively.
Moreover,
dihydroxyphenyl
triazene
5
demonstrated
3.03
5.66
12.50
Caco2,
HepG-2
Similarly,
carbohydrazide
coumarin
18
showed
of
2.00
12.30
HepG2,
Molecular
docking
using
hCAIX
hCAXII
adopted
explain
achieved
cytotoxicity
on
molecular
level
their
silico
ADME
evaluation.
RSC Medicinal Chemistry,
Journal Year:
2024,
Volume and Issue:
15(6), P. 1798 - 1827
Published: Jan. 1, 2024
Decades
ago,
the
application
of
cyclic
sulfonamide
(sultam)
and
its
derivatives
primarily
focused
on
their
antibacterial
properties.
However,
recent
years
have
seen
a
shift
in
research
attention
towards
exploring
potential
as
anticancer,
anti-inflammatory,
antidiabetic,
antiviral
agents.
Despite
this
broadening
scope,
only
few
sultam
drugs
made
it
to
commercial
market,
much
sultams
remains
discovery
phase.
This
class
compounds
holds
significant
promise
pertinent
pharmaceutical
research.
Due
sultam's
relevance
growing
importance
drug
discovery,
review
paper
aims
consolidate
examine
biological
activities
ranging
from
4
8-membered
ring
structures.
Arabian Journal of Chemistry,
Journal Year:
2023,
Volume and Issue:
16(8), P. 104956 - 104956
Published: May 3, 2023
New
thiadiazole
sulfonamide
derivatives
were
designed
as
human
carbonic
anhydrase
inhibitors
(hCAIs)
to
develop
robust
and
novel
anticancer
agents.
Tail
modification
approach
was
considered
in
designing
the
target
compounds
which
synthesized
following
two-step
procedure
starting
from
5-acetyl-3-N-(4-sulfamoylphenyl)-2-imino-1,3,4-thiadiazoline.
Cytotoxic
evaluation
revealed
potent
diazene
derivative
2
with
IC50
1.18
μM,
5.28
μM
7.15
against
MCF-7,
Caco2
HepG-2,
respectively.
Moreover,
dihydroxyphenyl
triazene
5
demonstrated
3.03
5.66
12.50
Caco2,
HepG-2
Similarly,
carbohydrazide
coumarin
18
showed
of
2.00
12.30
HepG2,
Molecular
docking
using
hCAIX
hCAXII
adopted
explain
achieved
cytotoxicity
on
molecular
level
their
silico
ADME
evaluation.