ChemistrySelect,
Journal Year:
2021,
Volume and Issue:
6(4), P. 685 - 694
Published: Jan. 25, 2021
Abstract
A
series
of
three
different
classes
benzothiazole
linked
1,2,3‐triazole
hybrid
molecules
with
varying
alkyl
spacers
(ethyl,
propyl,
and
butyl)
between
2‐hydroxyphenyl
benzothiazoles
1,2,3‐triazoles
are
efficiently
synthesized
under
CuAAC
condition.
All
compounds
satisfactorily
characterized
by
FTIR,
1
H‐NMR,
13
C‐NMR,
ESI‐MS
data
structures
some
were
finally
supported
single‐crystal
X‐ray
diffraction
data.
Most
the
exhibited
good
to
better
DNA
binding
property
(0.28×10
5
M
−1
2.91×10
)
well
drug‐like
properties.
Some
promising
showed
agreement
all
experimental
theoretical
computed
properties
(fluorescence
study,
binding,
molecular
docking,
DFT,
ADME
Predictions).
Current Topics in Medicinal Chemistry,
Journal Year:
2020,
Volume and Issue:
21(1), P. 59 - 72
Published: Oct. 23, 2020
Thiosemicarbazones
(TSCNs)
constitute
a
broad
family
of
compounds
(R
1
R
2
C=N-NH-C(S)-
NR
3
4
),
particularly
attractive
because
many
them
display
some
biological
activity
against
wide
range
microorganisms
and
cancer
cells.
Their
can
be
related
to
their
electronic
structural
properties,
which
offer
rich
set
donor
atoms
for
metal
coordination
high
delocalization
providing
different
binding
modes
biomolecules.
Heterocycles
such
as
pyrrole,
imidazole
triazole
are
present
in
molecules
Vitamine
B12
amino
acids
could
potentially
target
multiple
processes.
Considering
this,
we
have
explored
the
chemistry
properties
thiosemicarbazones
series
complexes
bearing
heterocycles
imidazole,
thiazole
triazole.
We
focus
at
cytotoxicity
those
derivatives
find
out
structure
relationships,
analyzed
examples
with
TSCN
units
mechanism
action
information
has
been
profoundly
studied
pathways
determined,
promote
future
studies
heterocycle
derivatives.
ACS Bio & Med Chem Au,
Journal Year:
2025,
Volume and Issue:
unknown
Published: Jan. 28, 2025
In
the
current
study,
we
report
synthesis
of
novel
4-((1-((1H-1,2,3-triazole-4-yl)methyl)-1H-indol-3-yl)methylene)-5-methyl-2-phenyl-2,4-dihydro-3H-pyrazole-3-one
derivatives
5a-o.
The
compounds
were
prepared
through
a
Knoevenagel
condensation
reaction
and
copper-catalyzed
azide-alkyne
cycloaddition
(CuAAC)
Click
chemistry
approach.
synthesized
exhibited
promising
antimicrobial
activity
against
both
Gram-positive
Gram-negative
bacteria.
Compounds
5e,
5h,
5i
displayed
potent
with
MIC
value
10
μg/mL
Acinetobacter
baumannii,
in
comparison
to
standard
drugs
chloramphenicol
ampicillin.
5d,
5i,
5l,
5m,
5n
good-to-moderate
antifungal
Candida
albicans
Aspergillus
niger
equivalent
nystatin
fluconazole.
this
cytotoxicity
profile
series
was
assessed
using
SHSY-5Y
cells.
results
indicate
that
5a-o
exhibit
no
significant
at
concentrations
up
100
μg/mL,
untreated
vehicle
control
groups.
These
findings
highlight
safety
tolerability
as
well
potential
effective
agents
bacterial
fungal
infections.
Journal of Biochemical and Molecular Toxicology,
Journal Year:
2025,
Volume and Issue:
39(3)
Published: March 1, 2025
ABSTRACT
Herein,
the
synthesis,
anticancer
activity
and
apoptotic
pathways
of
1,2,3‐triazolopyridazinones
compounds,
which
are
similar
to
DNA
bases
not
previously
found
in
literature
have
been
investigated.
To
achieve
this
goal,
it
is
designed
hybrid
molecules
combining
triazole
pyridazinone/pyridazithione
structures,
bearing
a
lipophilic
group
(benzyl/phenyl)
at
one
position
benzene
with
electron
withdrawing
or
donating
groups
five
positions,
high
pharmacophoric
properties
on
same
scaffold
structure.
The
representative
compounds
series
5a,
5c,
6a
8c
exhibited
higher
than
other
cisplatin
control
against
breast
(MCF‐7)
lung
(A549)
cell
lines.
These
were
less
toxic
when
tested
noncancerous
L929
line.
In
addition,
effect
mechanisms
these
confirmed
by
AO/EB
staining
caspase
3
results.
findings
indicate
that
some
derivatives
could
be
effective
therapeutic
agents
for
treatment
cancer
disease
an
apoptosis‐promoting.
