Targeting cancer using scaffold-hopping approaches: illuminating SAR to improve drug design
Drug Discovery Today,
Journal Year:
2024,
Volume and Issue:
29(9), P. 104115 - 104115
Published: July 26, 2024
Language: Английский
Unlocking the power of imidazoquinolines: recent advances in anticancer and immunotherapeutic strategies
Ranjini Jenifer R,
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Badruzzaman Choudhury,
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Mohammed Mujahid Alam
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et al.
Future Medicinal Chemistry,
Journal Year:
2025,
Volume and Issue:
unknown, P. 1 - 17
Published: April 15, 2025
The
challenges
in
drug
discovery
aiming
to
mitigate
cancer
progression
are
the
thrust
area
of
scientific
research
for
several
decades.
Since
advent
heterocyclic
chemistry,
programs
have
made
significant
achievements
that
lead
development
numerous
drugs
with
broad
spectrum
potencies,
contributing
both
diagnostic
and
therapeutic
advancements.
Till
date,
efforts
discover
more
potent
efficient
candidates
underway
minimize
adverse
side
effects
existing
chemotherapeutics.
In
view
above,
small-molecule
agonists
can
interact
different
immune
modulators
like
toll
receptor-7
(TLR-7)
TLR-8
being
investigated
explored.
These
expected
display
profound
effect
on
anti-tumoral
activity
by
enhancing
production
proinflammatory
cytokines.
Recently,
imidazoquinoline
derivatives
proven
TLR
agonist
activities
emerged
as
promising
anticancer
therapeutics.
With
advancements
technology
evolution
new
scopes
discovery,
strategies
adopted,
particularly
help
nanotechnology,
immune-technology,
combination
etc.,
curb
various
types
cancers.
Herein,
novel
therapeutics
imidazoquinolines
reported
last
5
years,
their
structure-activity
relationship
along
important
synthetic
schemes
agonists,
discussed.
Language: Английский
Vistas in the domain of 3-acetyl-4-hydroxy-2-quinolinone derivatives (AHQ) and their applications
Nedaa N. Elnaggar,
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Wafaa S. Hamama,
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Eslam A. Ghaith
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et al.
RSC Advances,
Journal Year:
2025,
Volume and Issue:
15(23), P. 18034 - 18088
Published: Jan. 1, 2025
This
review
discusses
the
significant
advances
in
current
status
and
latest
synthesis
techniques
for
N
-substituted
3-acetyl-4-hydroxyquinolinones.
Language: Английский
Special Issue: “Rational Design and Synthesis of Bioactive Molecules”
International Journal of Molecular Sciences,
Journal Year:
2024,
Volume and Issue:
25(18), P. 9927 - 9927
Published: Sept. 14, 2024
The
rational
design
of
novel
bioactive
molecules
is
a
critical
but
challenging
task
in
drug
discovery
[...]
Language: Английский
Synthesis of Thiaphenanthridinones from Sulfinate Esters and 2-Borylanilines
Organic Letters,
Journal Year:
2024,
Volume and Issue:
26(45), P. 9676 - 9681
Published: Nov. 6, 2024
A
facile
palladium-catalyzed
synthesis
of
thiaphenanthridinones
from
sulfinate
esters
and
2-borylanilines
is
disclosed.
Various
sulfur
analogs
phenanthridinones
were
synthesized
by
bromide-selective
cross-coupling
cyclization
in
one
step.
Further
transformations
the
obtained
allowed
preparing
a
broad
range
thiaphenanthridinone
derivatives
involving
bioactive
compounds.
Language: Английский
Synthesis of azaflavanones and alpha-ylidene azaflavanones
Tetrahedron,
Journal Year:
2024,
Volume and Issue:
167, P. 134295 - 134295
Published: Oct. 10, 2024
Language: Английский
One-Step Synthesis of 2-Arylquinolin-4(1H)-Ones from 1-(2-Aminoaryl)-3-Arylpropan-1-Ones via Pd(II)-Catalyzed Dehydrogenative Cyclization
Hyuck-Jae Won,
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Seung Hwan Son,
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Yo‐Sep Yang
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et al.
The Journal of Organic Chemistry,
Journal Year:
2024,
Volume and Issue:
90(1), P. 98 - 108
Published: Dec. 31, 2024
In
this
study,
we
developed
palladium-catalyzed
dehydrogenative
cyclization
to
transform
1-(2-aminoaryl)-3-arylpropan-1-ones
into
2-arylquinolin-4(1H)-ones,
also
known
as
aza-flavones
which
are
the
bioisosteres
of
flavones,
in
an
atom-economic
manner.
This
method
exhibited
excellent
chemical
compatibility
with
a
broad
substrate
scope,
accommodating
up
25
derivatives.
Additionally,
kinetic
studies
were
performed
elucidate
reaction
mechanism.
Further,
2-phenylquinolin-4(1H)-one
was
used
common
intermediate
for
synthesizing
privileged
structures
such
4-methoxyquinoline,
N-methylquinoline-4(1H)-one,
and
4-(pseudo)halogenated
quinoline
moieties.
Language: Английский