Studia Universitatis Moldaviae Seria Științe ale Naturii,
Год журнала:
2023,
Номер
1(171), С. 194 - 205
Опубликована: Сен. 1, 2023
In
this
article,
methods
of
synthesis
and
physicochemical
analysis
5
coordination
compounds
based
on
Cu(II)
ion
3-ethoxysalicylic
aldehyde
4-cyclohexyl-thiosemicarbazone
are
described.
the
first
step,
ligand
was
carried
out
by
means
two
classical
with
subsequent
refinement,
thus
obtaining
H2L
as
a
chelator
copper(II)
ions.
1H,
13C
15N-NMR
spectroscopy,
13C-DEPT-135
NMR
15N
HSQC-NMR
spectroscopy
were
applied
to
investigate
structure
geometry
4-cyclohexyl-thiosemicarbazone.
The
synthesized
substances
analyzed
modern
research
such
as:
FTIR
UV-vis
elemental
analysis,
single
crystal
X-ray
diffraction;
biological
activity
is
under
study.
Journal of Medicinal Chemistry,
Год журнала:
2023,
Номер
66(8), С. 5669 - 5684
Опубликована: Апрель 18, 2023
To
develop
the
next-generation
Pt
drug
with
remarkable
activity
and
low
toxicity
to
maximally
inhibit
tumor
growth,
we
optimized
a
Pt(II)
thiosemicarbazone
compound
(C4)
cytotoxicity
SK-N-MC
cells
then
constructed
new
human
serum
albumin-C4
(HSA-C4)
complex
delivery
system.
The
in
vivo
results
showed
that
C4
HSA-C4
have
therapeutic
efficiency
almost
no
toxicity;
they
induced
apoptosis
inhibited
angiogenesis.
This
system
potential
as
practical
drug.
study
could
pave
way
for
developing
dual-targeted
drugs
achieving
their
targeting
therapy
cancer.
New Journal of Chemistry,
Год журнала:
2023,
Номер
47(33), С. 15748 - 15759
Опубликована: Янв. 1, 2023
Michael
addition
derived
Pd(
ii
)
complexes
exhibited
potential
anticancer
activity
in
HeLa
cells
via
apoptosis.
In
vivo
models
showed
that
the
did
not
cause
any
harm
to
treated
mice,
portraying
better
selectivity
than
cisplatin.
Journal of Medicinal Chemistry,
Год журнала:
2024,
Номер
67(14), С. 12155 - 12183
Опубликована: Июль 5, 2024
We
implemented
isosteric
replacement
of
sulfur
to
selenium
in
a
novel
thiosemicarbazone
(PPTP4c4mT)
create
selenosemicarbazone
(PPTP4c4mSe)
that
demonstrates
potentiated
anticancer
efficacy
and
selectivity.
Their
design
specifically
incorporated
cyclohexyl
styryl
moieties
sterically
inhibit
the
approach
their
Fe(III)
complexes
oxy-myoglobin
heme
plane.
Importantly,
contrast
clinically
trialed
thiosemicarbazones
Triapine,
COTI-2,
DpC,
PPTP4c4mT
PPTP4c4mSe
did
not
induce
detrimental
oxidation.
Furthermore,
demonstrated
more
potent
antiproliferative
activity
than
homologous
thiosemicarbazone,
PPTP4c4mT,
with
selectivity
being
superior
or
similar,
respectively,
COTI-2.
An
advantageous
property
Zn(II)
relative
analogues
was
greater
transmetalation
Cu(II)
lysosomes.
This
latter
effect
probably
promoted
activity.
Both
ligands
down-regulated
multiple
key
receptors
display
inter-receptor
cooperation
leads
aggressive
resistant
breast
cancer.
Journal of Medicinal Chemistry,
Год журнала:
2024,
Номер
67(11), С. 9069 - 9090
Опубликована: Май 21, 2024
The
development
of
copper(II)
thiosemicarbazone
complexes
as
potential
anticancer
agents,
possessing
dual
functionality
inhibitors
R2
ribonucleotide
reductase
(RNR)
and
tubulin
polymerization
by
binding
at
the
colchicine
site,
presents
a
promising
avenue
for
enhancing
therapeutic
effectiveness.
Herein,
we
describe
syntheses
physicochemical
characterization
four
isomeric
proligands
Abstract
A
direct,
new
and
eco-friendly
strategy
for
the
one-step
synthesis
of
methoxylated
hydroxylated
styrenes
from
β-(phenyl)-β-(phenylthio)propionic
acids
is
reported.
This
approach
utilizes
a
neutral
ionic
liquid
[hmim]Br-triggered
cascade
decarboxylative
dehydrosulfenylation
reaction
under
microwave
irradiation,
without
need
strong
bases,
toxic
metal
oxidants,
eliminates
phenolic
group
protection–deprotection
strategy,
thus
offering
an
efficient
route
to
bio-based
commercially
important
FEMA
GRAS
approved
vinylphenols.
NMR
studies
suggest
concerted
mechanism.
Chemical Science,
Год журнала:
2023,
Номер
15(3), С. 974 - 990
Опубликована: Дек. 15, 2023
The
di-2-pyridylthiosemicarbazone
(DpT)
analogs
demonstrate
potent
and
selective
anti-proliferative
activity
against
human
tumors.
current
investigation
reports
the
synthesis
chemical
biological
characterization
of
Fe(iii),
Co(iii),
Ni(ii),
Cu(ii),
Zn(ii),
Ga(iii),
Pd(ii)
complexes
promising
second
generation
DpT
analog,
di-2-pyridylketone-4-ethyl-4-methyl-3-thiosemicarbazone
(Dp4e4mT).
These
studies
that
Dp4e4mT
display
distinct
Pharmacological Research,
Год журнала:
2023,
Номер
193, С. 106806 - 106806
Опубликована: Май 25, 2023
The
estrogen
receptor-α
(ER-α)
is
a
key
driver
of
breast
cancer
(BC)
and
the
ER-antagonist,
tamoxifen,
central
pillar
BC
treatment.
However,
cross-talk
between
ER-α,
other
hormone
growth
factor
receptors
enables
development
de
novo
resistance
to
tamoxifen.
Herein,
we
mechanistically
dissect
activity
new
class
anti-cancer
agents
that
inhibit
multiple
down-stream
signaling
for
treatment
ER-positive
BC.
Using
RNA
sequencing
comprehensive
protein
expression
analysis,
examined
di-2-pyridylketone-4,4-dimethyl-3-thiosemicarbazone
(Dp44mT)
di-2-pyridylketone-4-cyclohexyl-4-methyl-3-thiosemicarbazone
(DpC),
on
activation
receptors,
co-factors,
pathways
in
ER-α-positive
DpC
differentially
regulated
106
estrogen-response
genes,
this
was
linked
decreased
mRNA
levels
4
involved
pathogenesis,
namely
ER,
progesterone
receptor
(PR),
androgen
(AR),
prolactin
(PRL-R).
Mechanistic
investigation
demonstrated
due
Dp44mT
binding
metal
ions,
these
caused
pronounced
decrease
AR,
PR,
PRL-R
expression.
also
inhibited
epidermal
(EGF)
family
co-factors
promote
ER-α
transcriptional
activity,
including
SRC3,
NF-κB
p65,
SP1.
In
vivo,
highly
tolerable
effectively
growth.
Through
bespoke,
non-hormonal,
multi-modal
mechanisms,
PRL-R,
tyrosine
kinases
act
with
BC,
constituting
an
innovative
therapeutic
approach.
