Molecules,
Год журнала:
2024,
Номер
29(7), С. 1685 - 1685
Опубликована: Апрель 8, 2024
Two
new
phenylspirodrimanes,
stachybotrins
K
and
L
(1
2),
together
with
eight
known
analogues
(3–10),
were
isolated
from
deep-sea-derived
Stachybotrys
sp.
MCCC
3A00409.
Their
structures
determined
by
extensive
NMR
data
mass
spectroscopic
analysis.
Absolute
configurations
of
compounds
through
a
comparison
their
circular
dichroism
(CD)
spectra
other
reported
compounds.
The
possible
reversal
effects
all
assayed
in
the
resistant
cancer
cell
lines.
Stachybotrysin
B
(8)
can
reverse
multidrug
resistance
(MDR)
ABCB1-overexpression
cells
(KBv200,
Hela/VCR)
at
non-cytotoxic
concentration.
Doxorubicin
accumulation
assay
molecular-docking
analysis
reveal
that
mechanism
its
MDR
effect
may
be
related
to
increase
intracellular
concentration
substrate
anticancer
drugs.
RSC Advances,
Год журнала:
2024,
Номер
14(28), С. 19752 - 19779
Опубликована: Янв. 1, 2024
The
fluorinated
heterocycles
are
main
components
of
20%
the
anticancer
and
antibiotic
drugs,
this
review
describes
reported
antimicrobial
activities
five-membered
their
benzo-fused
systems.
Scientific Reports,
Год журнала:
2024,
Номер
14(1)
Опубликована: Янв. 2, 2024
Abstract
Chemotherapy
is
a
powerful
means
of
cancer
treatment
but
its
efficacy
compromised
by
the
emergence
multidrug
resistance
(MDR),
mainly
linked
to
efflux
transporter
ABCB1/P-glycoprotein
(P-gp).
Based
on
chemical
structure
betulin,
identified
in
our
previous
work
as
an
effective
modulator
P-gp
function,
series
analogs
were
designed,
synthesized
and
evaluated
source
novel
inhibitors.
Compounds
6g
6i
inhibited
rhodamine
123
overexpressed
leukemia
cells,
K562/Dox,
at
concentrations
0.19
µM
0.39
µM,
respectively,
increased
intracellular
accumulation
doxorubicin
submicromolar
concentration
0.098
µM.
able
restore
sensitivity
K562/Dox
Dox
0.024
respectively.
Structure–activity
relationship
analysis
molecular
modeling
revealed
important
information
about
structural
features
conferring
activity.
All
active
compounds
fitted
specific
region
involving
transmembrane
helices
(TMH)
4–6
from
one
homologous
half
TMH
7
12
other,
also
showing
close
contacts
with
6
12.
that
bound
preferentially
another
inactive,
regardless
their
free
energy
binding.
It
should
be
noted
devoid
toxic
effects
against
peripheral
blood
mononuclear
normal
cells
erythrocytes.
The
data
obtained
indicates
both
might
proposed
scaffolds
for
obtaining
promising
inhibitors
overcoming
MDR.
