Bioconjugate Chemistry,
Год журнала:
2024,
Номер
unknown
Опубликована: Дек. 31, 2024
The
dsDNA-selective
fluorescent-dye-based
DNA
damage
assay
was
developed
for
DNA-encoded
library
(DEL)
synthesis.
For
the
various
DEL
synthesis
conditions,
validated
through
cross-checking
with
high-performance
liquid
chromatography
(HPLC)
analysis,
and
fact
confirmed
that
usage
of
a
specific
ratio
organic
solvent
can
critically
induce
damage.
Also,
applicability
screening
DNA-damaging
condition
on-DNA
amide
coupling
reaction
Pd-catalyzed
N-arylation
reaction.
Organic Letters,
Год журнала:
2023,
Номер
26(13), С. 2517 - 2522
Опубликована: Дек. 18, 2023
The
increasing
role
of
the
DNA-encoded
library
technology
in
early
phase
drug
discovery
represents
a
significant
demand
for
DNA-compatible
synthetic
methods
therapeutically
relevant
heterocycles.
Herein,
we
report
first
on-DNA
synthesis
multisubstituted
indoles
via
cascade
reaction
Sonogashira
coupling
and
intramolecular
ring
closure.
Further
functionalization
by
Suzuki
at
third
position
exploits
diverse
chemical
space.
high
fidelity
method
also
enabled
construction
an
indole-based
mock
library.
Bioconjugate Chemistry,
Год журнала:
2024,
Номер
unknown
Опубликована: Дек. 31, 2024
The
dsDNA-selective
fluorescent-dye-based
DNA
damage
assay
was
developed
for
DNA-encoded
library
(DEL)
synthesis.
For
the
various
DEL
synthesis
conditions,
validated
through
cross-checking
with
high-performance
liquid
chromatography
(HPLC)
analysis,
and
fact
confirmed
that
usage
of
a
specific
ratio
organic
solvent
can
critically
induce
damage.
Also,
applicability
screening
DNA-damaging
condition
on-DNA
amide
coupling
reaction
Pd-catalyzed
N-arylation
reaction.
