Heterocycles‐Containing HDAC Inhibitors Active in Cancer: An Overview of the Last Fifteen Years
ChemMedChem,
Год журнала:
2024,
Номер
unknown
Опубликована: Авг. 29, 2024
Abstract
Cancer
is
one
of
the
primary
causes
mortality
worldwide.
Despite
nowadays
are
numerous
therapeutic
treatments
to
fight
tumor
progression,
it
still
challenging
completely
overcome
it.
It
known
that
Histone
Deacetylases
(HDACs),
epigenetic
enzymes
remove
acetyl
groups
from
lysines
on
histone's
tails,
overexpressed
in
various
types
cancer,
and
their
inhibition
represents
a
valid
strategy.
To
date,
some
HDAC
inhibitors
have
achieved
FDA
approval.
Nevertheless,
several
other
potential
drug
candidates
been
developed.
This
review
aims
primarily
be
comprehensive
studies
done
so
far
regarding
bearing
heterocyclic
rings
since
well
has
gained
increasing
interest
recent
years.
Hence,
inserting
moieties
HDAC‐inhibiting
scaffold
can
valuable
strategy
provide
potent
and/or
selective
compounds.
Here,
addition
summarizing
properties
novel
inhibiting
compounds,
we
also
ideas
for
developing
new,
more
potent,
compounds
treating
cancer.
Язык: Английский
A promising future for breast cancer therapy with hydroxamic acid-based histone deacetylase inhibitors
Bioorganic Chemistry,
Год журнала:
2025,
Номер
156, С. 108169 - 108169
Опубликована: Янв. 20, 2025
Язык: Английский
Hydroxamic and Poly(hydroxamic acids): A State-of-the-Art Review of Their Multifaceted Applications
Materials Today Communications,
Год журнала:
2025,
Номер
unknown, С. 111751 - 111751
Опубликована: Янв. 1, 2025
Язык: Английский
Discovery of novel biphenyl compounds bearing hydroxamic acid moiety as the first PD-L1/class I HDACs dual inhibitors
Journal of Enzyme Inhibition and Medicinal Chemistry,
Год журнала:
2025,
Номер
40(1)
Опубликована: Фев. 6, 2025
Herein,
we
firstly
reported
a
series
of
biphenyl
compounds
bearing
hydroxamic
acid
moiety
as
PD-L1/class
I
HDACs
dual
inhibitors.
Among
them,
compound
14
displayed
the
strongest
inhibitory
activity
in
vitro
against
HDAC2
and
HDAC3
with
IC50
values
27.98
nM
14.47
nM,
had
an
value
88.10
for
PD-1/PD-L1
interaction.
Importantly,
could
upregulate
expression
PD-L1
CXCL10
low-expression
cancer
cell
line
(MCF-7),
highlighting
potential
to
enhance
efficacy
by
recruiting
T-cell
infiltration
into
TME
improving
response
inhibitor
associated
low-expression.
Besides,
identified
another
compound,
22,
which
possessed
interaction
12.47
effectively
inhibited
proliferation
three
lines.
Our
results
suggest
that
22
can
be
served
lead
inhibitors
further
optimisation.
Язык: Английский
Small molecules targeting HDAC6 for cancer treatment: Current progress and novel strategies
Biomedicine & Pharmacotherapy,
Год журнала:
2024,
Номер
178, С. 117218 - 117218
Опубликована: Июль 30, 2024
Histone
deacetylase
6
(HDAC6)
plays
a
crucial
role
in
the
initiation
and
progression
of
various
cancers,
as
its
overexpression
is
linked
to
tumor
growth,
invasion,
migration,
survival,
apoptosis,
angiogenesis.
Therefore,
HDAC6
has
emerged
an
attractive
target
for
anticancer
drug
discovery
past
decade.
However,
development
conventional
inhibitors
been
hampered
by
their
limited
clinical
efficacy,
acquired
resistance,
inability
inhibit
non-enzymatic
functions
HDAC6.
To
overcome
these
challenges,
new
strategies,
such
dual-acting
inhibitors,
targeted
protein
degradation
(TPD)
technologies
(including
PROTACs,
HyT),
are
essential
enhance
activity
inhibitors.
In
this
review,
we
focus
on
recent
advances
design
modulators,
including
isoform-selective
HDAC6-based
dual-target
degraders
(PROTACs,
from
perspectives
rational
design,
pharmacodynamics,
pharmacokinetics,
status.
Finally,
discuss
challenges
future
directions
cancer
therapy.
Язык: Английский
Stimuli-Responsive Prodrugs with Self-Immolative Linker for Improved Cancer Therapy
Xu Wenting,
Ang Jia,
Zhixian Lei
и другие.
European Journal of Medicinal Chemistry,
Год журнала:
2024,
Номер
279, С. 116928 - 116928
Опубликована: Сен. 30, 2024
Язык: Английский
Design, Synthesis, and Biological Evaluation of HDAC Inhibitors Containing Natural Product-Inspired N-Linked 2-Acetylpyrrole Cap
Molecules,
Год журнала:
2024,
Номер
29(19), С. 4653 - 4653
Опубликована: Сен. 30, 2024
Drawing
inspiration
from
the
structural
resemblance
between
a
natural
product
Язык: Английский
Diversified applications and synthesis of hydroxamic acids
Australian Journal of Chemistry,
Год журнала:
2024,
Номер
77(12)
Опубликована: Дек. 6, 2024
Owing
to
the
ability
form
coordination
complexes
with
several
metal
ions,
hydroxamic
acids
have
been
widely
used
in
fields
of
medicinal
chemistry,
mineral
flotation,
metal–organic
frameworks
(MOFs),
remediation
contamination
and
more.
Since
three
acid-based
histone
deacetylase
(HDAC)
inhibitors
were
approved
by
US
Food
Drug
Administration
(FDA)
for
treatment
haematologic
malignancies,
such
functional
groups
acquired
even
more
attention
synthetic
chemistry.
However,
application
ore
beneficiation
is
a
unique
area
has
attracted
few
researchers.
In
order
provide
insights
chemists
drug
development,
chelating
collector
selection,
pollution
preparation
MOFs,
we
summarize
applications
above-mentioned
fields,
then
introduce
some
related
synthesis
strategies
including
microwave
synthesis,
use
continuous
flow
reactors,
solid-phase
enzymatic
as
supplements
classical
methods.
Язык: Английский