Journal of Inorganic Biochemistry,
Год журнала:
2024,
Номер
254, С. 112505 - 112505
Опубликована: Фев. 15, 2024
Platinum-based
anticancer
drugs,
while
potent,
are
associated
with
numerous
and
severe
side
effects.
Hyperthermia
therapy
is
an
effective
adjuvant
in
treatment,
however,
clinically
used
platinum
drugs
have
not
been
optimised
for
combination
hyperthermia.
The
derivatisation
of
existing
appropriately
chosen
thermoresponsive
moieties
results
being
activated
only
at
the
heated
site.
Perfluorinated
chains
varying
lengths
were
installed
on
carboplatin,
a
approved
drug,
leading
to
successful
synthesis
series
mono-
di-
substituted
platinum(IV)
carboplatin
prodrugs.
Some
these
complexes
display
relevant
thermosensitivity
ovarian
cancer
cell
lines,
i.e.,
inactive
37
°C
having
comparable
activity
under
mild
hyperthermia
(42
°C).
Nuclear
magnetic
resonance
spectroscopy
mass
spectrometry
indicated
that
likely
active
platinum(II)
agent
upon
reduction
cyclic
voltammetry
revealed
length
fluorinated
alkyl
chain
has
strong
influence
rate
formation,
regulating
subsequent
cytotoxicity.
Inorganic Chemistry Frontiers,
Год журнала:
2024,
Номер
11(11), С. 3085 - 3118
Опубликована: Янв. 1, 2024
The
reduction
of
Pt(
iv
)
complexes
can
be
monitored
by
various
analytical
techniques.
These
techniques
hold
significant
promise
in
elucidating
the
mechanisms
prodrug
activation,
aiding
rational
design
novel
prodrugs.
Journal of Inorganic Biochemistry,
Год журнала:
2024,
Номер
254, С. 112505 - 112505
Опубликована: Фев. 15, 2024
Platinum-based
anticancer
drugs,
while
potent,
are
associated
with
numerous
and
severe
side
effects.
Hyperthermia
therapy
is
an
effective
adjuvant
in
treatment,
however,
clinically
used
platinum
drugs
have
not
been
optimised
for
combination
hyperthermia.
The
derivatisation
of
existing
appropriately
chosen
thermoresponsive
moieties
results
being
activated
only
at
the
heated
site.
Perfluorinated
chains
varying
lengths
were
installed
on
carboplatin,
a
approved
drug,
leading
to
successful
synthesis
series
mono-
di-
substituted
platinum(IV)
carboplatin
prodrugs.
Some
these
complexes
display
relevant
thermosensitivity
ovarian
cancer
cell
lines,
i.e.,
inactive
37
°C
having
comparable
activity
under
mild
hyperthermia
(42
°C).
Nuclear
magnetic
resonance
spectroscopy
mass
spectrometry
indicated
that
likely
active
platinum(II)
agent
upon
reduction
cyclic
voltammetry
revealed
length
fluorinated
alkyl
chain
has
strong
influence
rate
formation,
regulating
subsequent
cytotoxicity.
