Yüzüncü Yıl Üniversitesi Tarım Bilimleri Dergisi,
Journal Year:
2023,
Volume and Issue:
33(3), P. 491 - 502
Published: Sept. 11, 2023
Natural
products
have
played
a
significant
role
in
drug
discovery
and
continue
to
be
an
important
source
of
lead
for
new
drugs.
In
recent
years,
computer-based
methods
emerged
as
effective
approach
identifying
small
molecule
leads
with
desirable
pharmacokinetic
toxicity
profiles.
This
study
investigated
the
pharmacological
bioactivity
five
furofuran
lignans,
namely,
epiexcelsin,
sesamin,
sesartemin,
syringaresinol,
yangambin,
isolated
from
plant
Beilschmiedia
pulverulenta.
silico
studies
were
conducted
predict
activities,
toxicity,
likeliness
properties
compounds.
The
results
showed
that
all
compounds
had
promising
epiexcelsin
exhibiting
strong
binding
affinity
(-8.13
kcal
mol-1)
inhibitory
activity
(1.1
µM)
against
estrogen
receptor-α,
predicted
bioavailable
lead.
findings
this
provide
insights
into
potential
therapeutic
uses
natural
medicinal
plants
emphasize
combining
traditional
knowledge
modern
scientific
approaches
discovery.
Overall,
lignans
pulverulenta
represent
development
International Journal of Molecular Sciences,
Journal Year:
2023,
Volume and Issue:
24(15), P. 12416 - 12416
Published: Aug. 4, 2023
Sixteen
new
thalidomide
analogs
were
synthesized.
The
candidates
showed
potent
in
vitro
antiproliferative
activities
against
three
human
cancer
cell
lines,
namely
hepatocellular
carcinoma
(HepG-2),
prostate
(PC3),
and
breast
(MCF-7).
It
was
found
that
compounds
XII,
XIIIa,
XIIIb,
XIIIc,
XIIId,
XIVa,
XIVb,
XIVc
IC50
values
ranging
from
2.03
to
13.39
µg/mL,
exhibiting
higher
than
all
tested
lines.
Compound
XIIIa
the
most
candidate,
with
an
of
±
0.11,
2.51
0.2,
0.82
0.02
µg/mL
compared
11.26
0.54,
14.58
0.57,
16.87
0.7
for
HepG-2,
PC3,
MCF-7
cells,
respectively.
Furthermore,
compound
reduced
expression
NFκB
P65
levels
HepG-2
cells
278.1
pg/mL
63.1
110.5
thalidomide.
Moreover,
induced
eightfold
increase
caspase-8
a
simultaneous
decrease
TNF-α
VEGF
cells.
Additionally,
apoptosis
cycle
arrest.
Our
results
reveal
are
potential
anticancer
candidates,
particularly
XIVc.
Consequently,
they
should
be
considered
further
evaluation
development
drugs.
Molecules,
Journal Year:
2023,
Volume and Issue:
28(7), P. 3239 - 3239
Published: April 5, 2023
Five
heterocyclic
derivatives
were
synthesized
by
functionalization
of
a
flavone
nucleus
with
an
aminophenoxy
moiety.
Their
cytotoxicity
was
investigated
in
vitro
two
models
human
non-small
cell
lung
cancer
(NSCLC)
cells
(A549
and
NCI-H1975)
using
MTT
assay
the
results
compared
to
those
obtained
healthy
fibroblasts
as
non-malignant
model.
One
(APF-1)
found
be
effective
at
low
micromolar
concentrations
both
lines
higher
selective
index
(SI).
Flow
cytometric
analyses
showed
that
APF-1
induced
apoptosis
cycle
arrest
G2/M
phase
through
up-regulation
p21
expression.
Therefore,
flavone-based
compounds
may
promising
cancer-selective
agents
could
serve
base
for
further
research
into
design
anticancer
drugs.
Current Green Chemistry,
Journal Year:
2023,
Volume and Issue:
11(2), P. 87 - 126
Published: Oct. 15, 2023
Abstract:
Organocatalysed
reactions
are
becoming
powerful
tools
in
the
construction
of
complex
molecular
skeletons.
It
gains
extra
importance
when
used
as
a
chemical
approach
to
fixation
carbon
dioxide
(CO2).
Carbon
is
an
increasingly
dangerous
environmental
hazard
global
climate
temperature
rises
through
greenhouse
effect.
Meanwhile,
past
decades,
significant
advances
can
be
noted
use
organocatalysis
for
CO2
capture
and
its
conversion
into
valuable
chemicals.
Therefore,
herein
we
review
full
set
organocatalysts
synthesis
N-heterocycles
since
they
present
several
structures
with
biological
relevance.
Al-Azhar Journal of Pharmaceutical Sciences/Al-Azhar Journal of Pharmaceutical Sciences,
Journal Year:
2024,
Volume and Issue:
69(1), P. 38 - 61
Published: March 1, 2024
Indoleamine-2,3-dioxygenase
(IDO)
and
tryptophan-2,3-dioxygenase
(TDO)
are
enzymes
that
catalyze
the
rate-limiting
step
of
kynurenine
pathway.
Recent
literature
reports
IDO
TDO
upregulation
in
tumor
cells
leading
to
L-tryptophan
depletion
accumulation
tryptophan
metabolites.
This
process
represents
an
essential
mechanism
for
tumor-induced
immunosuppression.
Following
failure
Epacadostat,
inhibitor,
phase
3
clinical
trials,
numerous
studies
have
shifted
a
dual
inhibition
scheme
overcome
compensation
linked
TDO.
Therefore,
using
single
molecule
emerges
as
highly
promising
therapeutic
approach.
comprehensive
review
aims
discuss
successful
scaffolds
reported
inhibitors
their
inhibitory
values
against
both
enzymes.
The
active
compounds
potential
form
novel
chemical
class
anti-tumor
immune
modulator
drugs.
