Frontiers in Chemistry,
Год журнала:
2024,
Номер
12
Опубликована: Фев. 19, 2024
This
comprehensive
review,
covering
2021-2023,
explores
the
multifaceted
chemical
and
pharmacological
potential
of
coumarins,
emphasizing
their
significance
as
versatile
natural
derivatives
in
medicinal
chemistry.
The
synthesis
functionalization
coumarins
have
advanced
with
innovative
strategies.
enabled
incorporation
diverse
functional
fragments
or
construction
supplementary
cyclic
architectures,
thereby
biological
physico-chemical
properties
compounds
obtained
were
enhanced.
unique
structure
coumarine
facilitates
binding
to
various
targets
through
hydrophobic
interactions
pi-stacking,
hydrogen
bonding,
dipole-dipole
interactions.
Therefore,
this
important
scaffold
exhibits
promising
applications
uncountable
fields
chemistry
(e.g.,
neurodegenerative
diseases,
cancer,
inflammation).
International Journal of Molecular Sciences,
Год журнала:
2023,
Номер
24(10), С. 8463 - 8463
Опубликована: Май 9, 2023
Currently,
polypropylene
(PP)
is
used
in
various
products,
thus
leading
to
high
daily
exposure
humans.
Thus,
it
necessary
evaluate
the
toxicological
effects,
biodistribution,
and
accumulation
of
PP
microplastics
human
body.
In
this
study,
administration
two
particle
sizes
(approximately
5
10-50
µm)
did
not
lead
any
significant
changes
several
evaluation
parameters,
including
body
weight
pathological
examination,
compared
with
control
group
ICR
mice.
Therefore,
approximate
lethal
dose
no-observed-adverse-effect
level
mice
were
established
as
≥2000
mg/kg.
Furthermore,
we
manufactured
cyanine
5.5
carboxylic
acid
(Cy5.5-COOH)-labeled
fragmented
monitor
real-time
vivo
biodistribution.
After
oral
Cy5.5-COOH-labeled
mice,
most
detected
gastrointestinal
tract
observed
be
out
after
24
h
IVIS
Spectrum
CT.
study
provides
a
new
insight
into
short-term
toxicity,
distribution,
mammals.
Molecules,
Год журнала:
2024,
Номер
29(19), С. 4534 - 4534
Опубликована: Сен. 24, 2024
Quorum
sensing
(QS)
is
a
bacterial
cell-to-cell
communication
mechanism
that
plays
an
essential
role
in
pathogenesis.
QS
governs
behavior
and
controls
biofilm
formation,
which
turn
contributes
to
antibiotic
resistance.
Therefore,
identifying
synthesizing
novel
compounds
overcome
inhibit
formation
are
essential.
Coumarins
important
plant-derived
natural
products
with
wide-ranging
bioactivities
extensive
applications,
including
antibacterial,
antifungal,
anticoagulant,
antioxidant,
anticancer,
anti-inflammatory
properties.
Additionally,
coumarins
capable
of
rewiring
inhibition,
leading
higher
susceptibility
antimicrobial
agents
less
this
review,
we
aim
provide
overview
formation.
This
review
also
discusses
the
synthesized
controlling
QS,
inhibiting
inducing
synergy
antibiotic–coumarin
combinations.
Hence,
emphasizes
potential
coumarin
act
as
antibacterial
demonstrates
their
ability
alleviate
Organic Letters,
Год журнала:
2023,
Номер
25(20), С. 3733 - 3738
Опубликована: Май 16, 2023
A
copper(II)-P,N,N-ligand
catalyzed
propargylic
[3
+
2]
cycloaddition
approach
for
the
synthesis
of
optically
enriched
dihydrofuro[3,2-c]coumarins
has
been
accomplished
first
time.
The
utilizes
esters
as
C2-bis-electrophiles
and
4-hydroxycoumarin
derivatives
C,O-bis-nucleophiles.
In
addition,
this
novel
strategy
was
also
explored
with
4-hydroxy-2-quinolinones
4-hydroxythiocoumarins.
Moreover,
various
their
quinolinone
thiocoumarin
analogues
were
synthesized
in
moderate
to
good
yields
high
enantioselectivities.
Scientific Reports,
Год журнала:
2025,
Номер
15(1)
Опубликована: Фев. 24, 2025
Microplastics
(MPs),
plastic
particles
with
a
diameter
of
<
5
mm,
are
intentionally
produced
or
formed
by
the
breakdown
variety
larger
plastics.
Polyethylene
terephthalate
(PET)
is
common
source
MPs
and
PET-MPs
prevalent
in
environment.
Owing
to
their
persistence,
can
enter
ecosystems,
air,
food
sources,
posing
significant
health
risks.
This
study
aimed
investigate
toxicological
effects
vivo
accumulation
smaller
than
10
µm.
To
track
biodistribution,
fluorescently
labeled
were
prepared.
Particle
size
morphology
confirmed
using
physical
chemical
characterization.
Following
oral
administration
ICR
(CD-1®)
outbred
mice,
occurred
predominantly
lungs,
as
IVIS
spectrum
CT
analysis
ex
imaging.
Toxicity
assays
revealed
development
granulomatous
inflammation
lungs
at
medium
high
doses,
indicating
concentration-dependent
response.
The
recorded
no-observed-adverse-effect
levels
1.75
mg/kg
for
males
7
females.
highlights
potential
induce
persistent
respiratory
tissues
reveals
need
further
research
support
regulatory
standards
long-term
MP
exposure.
Current Organocatalysis,
Год журнала:
2024,
Номер
11(4), С. 321 - 329
Опубликована: Фев. 2, 2024
Background:
MCRs
are
one
of
the
most
significant
tools
in
synthesis
organic
compounds.
MCR
is
a
rapid
chemical
technique
that
uses
three
or
more
reactants
to
produce
products
sustain
all
structural
and
substructural
properties
initial
components.
useful
fields
synthetic
chemistry
because
their
rate
reaction,
simple
procedure
excellent
yields.
We
reported
an
efficient
environmentally
friendly
domino
approach
for
spiroheterocycles
spiro
annulated
with
indeno[1,2-b]quinoline.
Method:
The
privileged
heterocyclic
substructures
have
been
synthesized
using
taurine
(2-aminoethanesulfonic
acid)
as
green,
sustainable,
bio-organic
recyclable
catalyst
three-component
reaction
isatins,
1,3-diketones,
1-napthylamine
aqueous
media.
present
method
probably
first
report
synthesize
spiroheterocycles,
spiroannulated
Furthermore,
valuable
yield
results
from
15-20
min.
Result:
optimization
conditions
important
case
synthesis.
solvent,
temperature,
time
loading
were
examined.
reusability
was
also
investigated
experimentally.
used
has
high
activity
well
good
reusability.
protocol
will
be
extended
synthesise
library
hybrid
cost-effective,
time-efficient
easy-workup
methodology
gives
outstanding
yields
(80–95%)
15–20
Conclusion:
Taurine-catalyzed
multicomponent
novel
indeno[1,2-b]quinolines.
catalytic
water
green
solvent
makes
process
friendly.
special
features
include
efficiency,
operational
simplicity,
it
expected
make
contributions
not
only
drug
discovery
studies
but
pharmaceutical
therapeutic
view
introducing
molecular
diversity
molecules.
Organic & Biomolecular Chemistry,
Год журнала:
2024,
Номер
unknown
Опубликована: Янв. 1, 2024
The
regioselective
1,2-dicarbonylation
of
aryls
and
heteroaryls
offers
access
to
functionalized
dicarbonylated
heteroaryls,
which
opens
pharmaceuticals
bioactive
molecules
with
diverse
synthetic
utility.
ACS Omega,
Год журнала:
2024,
Номер
9(2), С. 2286 - 2301
Опубликована: Янв. 3, 2024
Epidermal
growth
factor
receptor
(EGFR)-targeted
therapy
has
been
proven
vital
in
the
last
two
decades
for
treatment
of
multiple
cancer
types,
including
nonsmall
cell
lung
cancer,
glioblastoma,
breast
and
head
neck
squamous
carcinoma.
Unfortunately,
majority
approved
EGFR
inhibitors
fall
into
drug
resistance
category
because
continuous
mutations
acquired
resistance.
Recently,
autophagy
surfaced
as
one
emerging
underlying
mechanisms
behind
to
EGFR-tyrosine
kinase
(TKIs).
Previously,
we
developed
a
series
4″-alkyl
EGCG
(4″-Cn
EGCG,
n
=
6,
8,
10,
12,
14,
16,
18)
derivatives
with
enhanced
anticancer
effects
stability.
Therefore,
current
study
hypothesized
that
might
induce
cytoprotective
upon
inhibition,
inhibition
may
lead
improved
cytotoxicity.
In
this
study,
have
observed
caspase-3-dependent
apoptosis
derivative-treated
glioblastoma
cells
(U87-MG).
We
also
confirmed
could
inhibit
cells,
well
mutant
L858R/T790M
EGFR,
through
an
vitro
assay.
Furthermore,
found
induces
autophagic
responses,
accompanied
by
blockage
AKT/mTOR
signaling
pathway.
addition,
cytotoxicity
caused
4″-C10
4″-C12
4″-C14
was
significantly
increased
after
pharmacological
inhibitor
chloroquine.
These
findings
enhance
our
understanding
response
toward
suggest
potent
combinatorial
strategy
increase
therapeutic
effectiveness
EGFR-TKIs.
Abstract
Being
an
important
constituent
of
naturally
occurring
heterocyclic
compounds
with
a
myriad
interesting
biological
activities,
the
furocoumarin
motif
has
claimed
vast
interest
in
synthetic
and
medicinal
research.
Designing
organic
synthesis
following
green
sustainable
approach
finds
special
importance
terms
energy
efficiency,
cost‐effectiveness
hence
becoming
domain
research
recent
past.
The
methodologies
for
presented
here
particularly
include
strategies
developed
under
microwave
irradiation,
solvent‐free
conditions
or
uses
solvent,
metal‐free
routes,
room
temperature
mediated
one‐pot
MCR
reactions.
This
review
article
attempts
to
highlight
advances
furocoumarins
along
general
aspects
like
natural
occurrence,
activities
this
particular
scaffold.
