Results in Chemistry,
Год журнала:
2024,
Номер
7, С. 101494 - 101494
Опубликована: Янв. 1, 2024
Various
pharmacological
properties
of
coumarins
brought
them
under
light
among
the
heterocyclics.
Also,
coumarin
derivatives
still
approve
their
importance
in
medical
field
as
a
valuable
building
block
to
elicit
further
with
diverse,
potent,
and
interesting
biological
activities.
Moreover,
numerous
actions
thiadiazole-based
compounds
contribute
notion
this
unique
synthesis
linearly
fused
thiadiazolocoumarins
using
molecular
hybridization
method.
This
work
reported
novel
seven
thiadiazolocoumarins,
including
Precursor
N-III
TDA1-TDA6.
These
were
characterized
by
physicochemical
through
spectrophotometric
tools,
FTIR,
1H
NMR,
13C
NMR.
pharmacokinetics
predicted
computer-based
studies
SwissADME
PreADMET
programs.
Furthermore,
checked
for
several
activities,
anticancer,
biosafety,
anti-oxidative
stress,
anti-inflammatory,
antimicrobial,
normal
flora
safety,
antidiabetic
According
results,
TDA3
showed
greatest
anticancer
activity
against
examined
cancer
cell
lines,
highest
cellular
biosafety.
TDA4
higher
stress
than
other
derivatives.
All
prepared
significant
inflammation-inhibitory
toward
LOX-5
enzyme
while
showing
poor
towards
COX
enzymes.
antimicrobial
activity,
exhibited
anti-gram-negative
also
best
safety
flora.
TDA1
promising
anaerobic
bacteria,
N-III,
TDA3,
antifungal
activity.
Finally,
demonstrated
moderate
which
was
The
authors
concluded
from
gathered
results
that
represent
key
structures
developing
versatile
bioactivities.
Results in Chemistry,
Год журнала:
2024,
Номер
8, С. 101611 - 101611
Опубликована: Июнь 1, 2024
Despite
the
up-to-date
advancements
in
its
treatment,
cancer
is
still
being
harvested
lives
of
millions
people
annually;
this
health
threat
necessitates
exploring
more
potent
agents
that
can
effectively
fight
it.
The
class
heterocycles
known
as
coumarin,
and
natural
synthetic
derivatives
are
thought
to
be
biomedically
valuable.
Coumarins
have
low
side
effects,
outstanding
selectivity,
a
straightforward
design
for
maximum
efficiency,
various
pharmacological
actions.
For
these
characteristics,
coumarins
continuously
isolated
from
sources
synthesized
laboratories,
alongside
with
examining
them
possible
bioactivities.
In
addition
garnering
significant
attention,
coumarin
has
emerged
valuable
scaffold
potentially
important
precursor
development
innovative
anticancer
medicines.
Researchers
working
create
new
cancer-fighting
coumarins,
well
investigating
old
ones.
Integration
two
or
cyclic
moieties
into
single
molecular
framework
might
enhance
existing
effects
perhaps
provide
entirely
Numerous
studies
shown
synergistic
additive
impact
when
fused
where
fusion
may
occur
at
coumarin-benzene
coumarin-lactone.
current
paper
explores
detail
how
linearly
ring-fused
combat
cancer.
derivative
number
42
was
determined
best
among
were
reviewed.
Compared
5-flourouracil,
IC50
values
against
six
cell
lines
promising.
These
25.08,
13.42,
41.45,
28.43,
31.15,
13.08
μM
SK-OV-3,
HeLa,
KYSE-30,
AMN3,
SKG,
MCF-7,
respectively.
attribute
obvious
compared
those
reference,
which
following
same
order
lines:
22.43,
13.37,
30.72,
24.89,
22.12,
12.42
μM.
researchers
conducted
searches
across
multiple
data
repositories,
such
Scopus,
Google
Scholar,
Web
Science,
PubMed.
After
conducting
thorough
analysis,
authors
found
included
59
pertinent
publications
published
by
end
2023.
reviewed
help
medicinal
chemists
manufacture
functionally
active
leads
using
scaffolds
been
mentioned.
knowledge
derived
offer
substantial
medical
benefits
short
term
powerful
drugs
could
boost
chemotherapeutics.
Chemistry & Biodiversity,
Год журнала:
2024,
Номер
unknown
Опубликована: Июль 16, 2024
Abstract
Acetaminophen,
a
centrally‐acting
old
analgesic
drug,
is
weak
inhibitor
of
cyclooxygenase
(COX)
isoforms
with
some
selectivity
toward
COX‐2.
This
compound
was
used
in
this
work
as
precursor
to
create
nine
acetaminophen
based
coumarins
(ACFs).
To
satisfy
the
aim
work,
which
states
synthesis
acetaminophen‐based
selective
COX‐2
inhibitors,
ACFs
were
subjected
two
types
investigation:
vitro
and
silico
.
Given
former
type,
capacity
block
COX‐1
investigated
lab
settings.
On
other
hand,
investigation
included
docking
chemical
structures
into
active
sites
these
enzymes,
predicting
their
anticipated
toxicities,
determining
ADME
characteristics.
The
results
study
revealed
that
synthesized
demonstrated
good‐to‐excellent
inhibitory
properties
against
enzymes
under
study.
Also,
exhibited
high
level
selectivity,
improved
aromatic
substitute
for
withdrawing
electrons
enhanced.
Results
comparable
case
investigations
indicated
are
safer
than
precursor,
acetaminophen,
potential
consider
oral‐administrated
candidates.
