Exploring 1,2,3-triazole-Schiff’s base hybrids as innovative EGFR inhibitors for the treatment of breast cancer: In vitro and in silico study
Bioorganic Chemistry,
Год журнала:
2025,
Номер
155, С. 108106 - 108106
Опубликована: Янв. 4, 2025
Язык: Английский
Fused Imidazo[1,2‐d][1,2,4]Thiadiazolo[1,2,3]Triazoles: One‐Pot Synthesis, Anti‐Bacterial, Anti‐Biofilm and TLR4 Inhibitory Activities
ChemistrySelect,
Год журнала:
2024,
Номер
9(32)
Опубликована: Авг. 23, 2024
Abstract
We
developed
and
evaluated
several
new
fused
imidazo[1,2‐d][1,2,4]thiadiazolo[1,2,3]triazoles
to
see
how
they
perform
against
bacteria
biofilms.
Some
compounds
showed
acceptable
activity
compared
the
primary
standard,
Dicloxacillin.
of
demonstrated
significant
antibacterial
S.
aureus
,
with
MIC
values
ranging
from
1.56–12.5
μg/mL.
also
found
anti‐biofilm
properties
in
potent
compounds.
The
results
that
derivatives
3‐(4‐fluorophenyl)imidazo[1,2‐d]
[1,2,3]
triazolo[1,5‐b][1,2,4]thiadiazole
8,8‐dioxide
3‐(3,5‐difluorophenyl)imidazo[1,2‐d][1,2,3]triazolo[1,5‐b][1,2,4]
thiadiazole
were
strong
agents
effective
MSSA
MRSA
biofilm
growth
inhibitors.
conducted
silico
studies
assess
molecular
interactions
more
TLR4
proteins
(PDB:
3FXI,
3VQ1,
3RG1).
Our
findings
revealed
3‐(4‐chloro‐3,5‐dimethoxyphenyl)imidazo[1,2‐d][1,2,3]triazolo[1,5‐b]
[1,2,4]thiadiazole
8,8‐dioxide,
3‐(3,5‐dichlorophenyl)imidazo[1,2‐d]
[1,2,3]triazolo[1,5‐b][1,2,4]
3‐(4‐(trifluoromethyl)phenyl)imidazo[1,2‐d][1,2,3]triazolo[1,5‐b][1,2,4]
exhibited
binding
than
dicloxacillin.
ADME
examined
this
study
could
potentially
inhibit
cytochrome
P450
CYP2C19
isoform.
Язык: Английский
One‐Pot Synthesis of Fused Isoxazolo[4′,5′:3,4]pyrrolo[2,1‐b] Quinazolines as Potent EGFR Targeting Anticancer Agents
ChemistrySelect,
Год журнала:
2024,
Номер
9(40)
Опубликована: Окт. 1, 2024
Abstract
In
response
to
the
need
for
scaffolds
medical
applications,
synthetic
chemists
have
developed
simple
and
efficient
methods
optimal
synthesis.
To
investigate
synthesis
of
fused
isoxazoles
in
presence
[3+2]
cycloaddition
followed
by
C−N
bond
formation
reaction
between
3‐((4‐iodo‐3‐phenylisoxazol‐5‐yl)methyl)quinazolin‐4(3H)‐one
various
nitrile
oxides
was
carried
out
previously
reported
conditions.
The
cancer
activities
synthesized
compounds
were
then
tested
vitro
against
two
cell
lines,
MCF‐7
A‐549.
Three
compounds,
3‐(3,5‐dichlorophenyl)
isoxazolo[4′,5′:3,4]pyrrolo[2,1‐b]quinazolin‐9(11H)‐one,
3‐(4‐fluorophenyl)isoxazolo[4′,5′:3,4]pyrrolo[2,1‐b]quinazolin‐9(11H)‐one,
3‐(4‐(trifluoromethyl)phenyl)isoxazolo[4′,5′:3,4]
pyrrolo[2,1‐b]
quinazolin‐9(11H)‐one
has
shown
superior
activity
non‐small‐cell
lung
line
(A‐549)
than
standards
5‐fluorouracil
erlotinib.
Later,
EGFR
results
revealed
that
a
more
potent
compound
effective
conventional
medicine,
silico
investigations
erlotinib
on
protein
indicated
had
comparable
binding
energies
inhibition
constants
Язык: Английский
Utilizing perhalopyridine-based alkynes as suitable precursors for the synthesis of novel poly(1,2,3-triazolyl)-substituted perhalopyridines
RSC Advances,
Год журнала:
2024,
Номер
14(42), С. 30873 - 30885
Опубликована: Янв. 1, 2024
A
novel
series
of
poly(1,2,3-triazolyl)-substituted
perhalopyridines
were
synthesized
under
ultrasonic
irradiation.
We
also
developed
an
effective
method
for
the
preparation
((1,2,3-triazol-4-yl)methoxy)-3,4,5,6-tetrachloropyridines.
Язык: Английский
One-pot synthesis of fused isoxazolo[4′,5′:4,5]thiopyrano[2,3-d]pyrimidines as potent EGFR targeting anti-lung cancer agents
Suresh S. Ardhapure,
Shivraj B. Sirsat
Tetrahedron Letters,
Год журнала:
2024,
Номер
unknown, С. 155325 - 155325
Опубликована: Окт. 1, 2024
Язык: Английский
Synthesis of New Imidazolo‐Benzenesulfonamide Linked 1,2,3‐Triazoles as Potent Antibacterial and Antibiofilm Agents
ChemistrySelect,
Год журнала:
2024,
Номер
9(38)
Опубликована: Окт. 1, 2024
Abstract
In
search
of
better
antibacterial
and
antibiofilm
agents,
this
report
presents
a
series
novel
1,2,3‐triazole‐imidazole‐benzenesulfonamide
derivatives
that
were
synthesized
evaluated
for
their
activity
in
vitro.
Antibacterial
against
three
Gram‐positive
bacterial
strains,
B.
subtilis
,
S.
aureus
epidermidis
was
evaluated.
Among
all
the
tested
compounds,
4‐methyl‐
N
‐(1‐methyl‐1
H
‐imidazol‐2‐yl)‐
‐((1‐(4‐(trifluoromethyl)phenyl)‐1
‐1,2,3‐triazol‐4‐yl)methyl)benzenesulfonamide
‐((1‐(3,5‐difluorophenyl)‐1
‐1,2,3‐triazol‐4‐yl)methyl)‐4‐methyl‐
‐imidazol‐2‐yl)benzenesulfonamide
exhibited
potent
strains.
Biofilm
profiles
compounds
it
observed
from
results
above
two
active
displayed
promising
biofilm
inhibition
with
MIC
values
ranging
between
2.19
±
0.37
3.38
0.35
µg/mL.
Furthermore,
screened
silico
molecular
docking
studies
penicillin‐binding
protein
compound
‐((1‐(3,5‐dichlorophenyl)‐1
show
highest
binding
energy
as
compared
to
standard
remaining
compounds.
Язык: Английский