A new framework for novel analogues of pazopanib as potent and selective human carbonic anhydrase inhibitors: Design, repurposing rational, synthesis, crystallographic, in vivo and in vitro biological assessments
European Journal of Medicinal Chemistry,
Год журнала:
2024,
Номер
274, С. 116527 - 116527
Опубликована: Май 24, 2024
Язык: Английский
Synthesis of thiazolidine-2,4-dione tethered 1,2,3-triazoles as α-amylase inhibitors: In vitro approach coupled with QSAR, molecular docking, molecular dynamics and ADMET studies
European Journal of Medicinal Chemistry,
Год журнала:
2024,
Номер
275, С. 116623 - 116623
Опубликована: Июнь 25, 2024
Язык: Английский
Phosphorus-Nitrogen Compounds: Part 79. Design and synthesis of spiro-bino-spiro (sbs)-bis (tetraalkylaminocyclotriphosphazenes) and novel twenty-membered bis(dichlorocyclotriphos-phaza)macrocycles: Structural analysis, chirality and bioactivity studies
Journal of Molecular Structure,
Год журнала:
2025,
Номер
unknown, С. 141926 - 141926
Опубликована: Март 1, 2025
Язык: Английский
Innovative Multitarget Organoselenium Hybrids With Apoptotic and Anti‐Inflammatory Properties Acting as JAK1/STAT3 Suppressors
Drug Development Research,
Год журнала:
2025,
Номер
86(2)
Опубликована: Март 18, 2025
ABSTRACT
Herein,
we
report
the
design,
synthesis,
and
characterization
of
novel
organoselenium
(OSe)
hybrids
(
5
–
19
)
via
modifications
lead,
N
‐(4‐selaneylphenyl)‐2‐selaneylacetamide.
The
OSe‐based
thiazol
9
showed
highest
growth
inhibition
%
(GI%)
64.72%
relative
to
positive
reference
doxorubicin
(DOX),
with
a
GI%
79.5%.
Furthermore,
OSe
derivatives
low
values
compared
normal
cell
lines
employed,
demonstrating
their
selectivity.
tethered
‐chloroacetamide
Schiff
base
cytotoxic
effect
an
IC
50
(25.07
11.61
µM),
respectively,
against
A549
tumor
line
(34.22
20.12
HELA
cancer
line.
Enzyme‐linked
immunosorbent
assay
study
JAK1
STAT3
inhibitory
potentials
compounds
in
cells
both
promising
activities
25.07
µM,
respectively.
Protein
expression
analysis
on
upregulation
P53,
BAX,
Caspases
3,
6,
8,
as
apoptotic
proteins.
However,
candidates
expressed
downregulation
antiapoptotic
proteins
(BCL2,
MMP2,
MMP9).
Moreover,
described
examined
inflammatory
proteins:
COX2,
IL‐6,
IL‐1β.
In
addition,
compound
potential
cycle
arrest
at
G0,
S,
G2‐M
layers,
increase
cellular
levels.
Finally,
molecular
docking
studies
most
toward
target
receptors,
binding
scores
interactions
exceeding
that
cocrystallized
inhibitor
JAK1.
Язык: Английский
Targeting DNA repair mechanisms: Spirobenzoxazinone and salicylamide derivatives as novel candidates for PARP-1 inhibition in cancer therapy
Bioorganic & Medicinal Chemistry,
Год журнала:
2025,
Номер
unknown, С. 118173 - 118173
Опубликована: Март 1, 2025
Язык: Английский
Pyridazinone based derivatives as anticancer agents endowed with anti-microbial activity; Molecular design, synthesis, and biological investigation
RSC Medicinal Chemistry,
Год журнала:
2024,
Номер
15(10), С. 3529 - 3557
Опубликована: Янв. 1, 2024
Discovery
of
novel
pyridazinone
derivatives
with
dual
antimicrobial
and
anticancer
activities.
Язык: Английский