On-DNA Medicinal Chemistry: Focused Libraries, Fragment Expansion, and Hit Optimisation
Royal Society of Chemistry eBooks,
Год журнала:
2025,
Номер
unknown, С. 87 - 118
Опубликована: Фев. 21, 2025
Since
their
inception
thirty
years
ago,
DNA-encoded
libraries
(DELs)
have
proven
to
be
a
formidable
technique
for
naïve
hit
finding,
with
implementation
facilitating
the
generation
of
lead-series
across
wide
range
target
classes.
In
recent
however,
it
has
been
demonstrated
that
utility
DELs
within
drug
discovery
need
not
restricted
this
purpose,
variety
strategies
being
adopted
broaden
impact
encoded
field.
Discussed
herein
are
current
applications
wider
medicinal
chemistry
pipeline,
including
application
and
focused
libraries;
use
fragment
expansion;
potential
facilitation
optimisation
processes.
The
state
field
is
assessed,
future
directions
technology
area
explored.
Язык: Английский
Photoinduced Site-Selective Alkylation Enabling Synthesis of C-3-Alkylated Quinoxalinone on DNA
Kyeong Seop Kim,
Junseok Ra,
Madala Hari Babu
и другие.
Organic Letters,
Год журнала:
2025,
Номер
unknown
Опубликована: Апрель 30, 2025
A
mild
and
biocompatible
strategy
for
the
site-selective
alkylation
of
quinoxalinones
via
photoinduced
dehydrogenative
has
been
developed.
This
protocol
enables
functionalization
both
unprotected
quinoxalinone
nonreactive
dihydroquinoxalinone
under
DNA-compatible
conditions.
The
optimized
reaction
proceeds
efficiently
while
tolerating
a
diverse
range
alkyl
donors
from
various
radical
precursors.
Given
its
simplicity
DNA
compatibility,
this
methodology
offers
platform
construction
DNA-encoded
libraries
incorporating
privileged
scaffold.
Язык: Английский
On-DNA Mannich Reaction for DNA-Encoded Library Synthesis
The Journal of Organic Chemistry,
Год журнала:
2024,
Номер
89(22), С. 16957 - 16963
Опубликована: Ноя. 1, 2024
The
β-amino
ketones
produced
through
the
Mannich
reaction
hold
significant
potential
as
candidates
for
various
drugs.
In
this
study,
we
optimized
on-DNA
conditions
and
applied
them
to
investigate
reactions
of
DNA-conjugated
aldehydes
with
amine
ketone
building
blocks.
developed
preserved
DNA
integrity
established
viable
routes
library
production.
These
results
underscore
in
DNA-encoded
(DEL)
synthesis.
Язык: Английский