Abstract
Eight
novel
compounds
incorporating
chalcone
and
coumarin
features,
namely
chalcone‐coumarin‐
hybrid
molecules,
were
designed,
synthetized,
evaluated
for
their
activity
against
human
colorectal
carcinoma
SW480
cell
line.
According
to
the
results
observed,
with
a
2,3‐dimetoxysubstitution
pattern
displayed
highest
at
conditions
evaluated,
an
IC
50
value
of
25.18±1.12
μM,
being
even
more
active
than
reference
drug
(5‐fluorouracil)
parental
compound
(7‐methylcoumarin).
In
addition,
this
exhibited
significant
antiproliferative
in
time‐
concentration
dependent
way,
suggesting
rather
cytostatic
or
cytotoxic
effect.
Moreover,
theoretical
drug‐like/pharmacokinetics/toxicological
study
suggested
that
most
promising
would
have
great
chance
advance
further
preclinical
studies
as
anti‐cancer
therapeutic
candidate
oral
oncological
management.
Our
evidently
identified
potency
chalcone‐coumarin
conjugates,
particularly
2,3‐dimetoxysubstituited
molecule
be
prototype
investigations
toward
therapeutics
treatments
cancer.
Archiv der Pharmazie,
Год журнала:
2024,
Номер
357(9)
Опубликована: Июнь 12, 2024
Among
ruthenium
complexes
studied
as
anticancer
metallodrugs,
NKP-1339,
NAMI-A,
RM175,
and
RAPTA-C
have
already
entered
clinical
trials
due
to
their
potent
antitumor
activity
demonstrated
in
preclinical
studies
reduced
toxicity
comparison
with
platinum
drugs.
Considering
the
advantages
of
ruthenium-based
drugs
cytostatic
organometallic
triazole-
coumarin-derived
ligands,
we
set
out
synthesize
Ru(II)
coumarin-1,2,3,-triazole
hybrids
(L)
general
formula
[Ru(L)(p-cymene)(Cl)]ClO
Chemistry - A European Journal,
Год журнала:
2024,
Номер
unknown
Опубликована: Июль 1, 2024
A
series
of
fluorescent
carbazole-coumarins
exhibiting
good
photoluminescence
quantum
yields
and
thermally
activated
delayed
fluorescence
(TADF)
properties
have
been
designed
synthetized
using
computer-aided
density
functional
theory
calculations.
The
TADF
characteristics
the
were
systematically
explored
both
in
solution
solid
state,
utilizing
poly(methyl
methacrylate)
(PMMA)
as
a
matrix.
study
revealed
that
introduction
carbazole
units
onto
coumarin
benzene
ring
led
to
compounds
with
induced
reverse
intersystem
crossing
fluorescence.
further
demonstrated
potential
utility
these
practical
applications
by
incorporating
them
into
Cmr-PMMA-based
sensor
for
molecular
oxygen
detection.
resulting
exhibited
promising
performance,
highlighting
adaptability
efficacy
synthesized
TADF-carbazole-coumarin
reversible
sensing.
