Design, Synthesis, and Biological Evaluation of Aryl Pyrazolopyrimidines as Toll‐Like Receptor 7 Agonists
Chemical Biology & Drug Design,
Journal Year:
2025,
Volume and Issue:
105(2)
Published: Jan. 30, 2025
ABSTRACT
Compounds
containing
pyrazolopyrimidine
scaffolds
were
designed
and
synthesized
as
toll‐like
receptor
7
(TLR7)
agonists.
Thirty‐three
compounds,
including
22
novel
prepared,
their
structures
identified
using
nuclear
magnetic
resonance
spectroscopy
mass
spectrometry.
TLR7
agonist
activity
was
determined
in
HEK‐Blue
hTLR7
reporter
cells.
Among
the
compounds
tested,
2‐((4‐methoxyphenyl)amino)‐7‐(pyridin‐2‐yl)pyrazolo[1,5
‐a
]pyrimidine‐3‐carbonitrile
showed
highest
activity,
further
vitro
biological
experiments
performed
this
compound.
Treatment
with
title
compound
activated
TLR7‐mediated
NF‐κB
pathway,
triggering
IRAK4‐IKKα/β‐IκBα‐p65
signaling
cascade,
which
led
to
an
increase
expression
of
NF‐κB‐regulated
innate
cytokines
such
TNFα
IL‐1β
RAW264.7
macrophages.
These
findings
suggest
that
acts
a
enhances
immune
response.
Language: Английский
Synthesis of Aryl Naphthoquinones and Maleimides via Pd(II)‐Catalyzed Template‐Assisted m‐C(sp2)‐H Functionalization Reaction
Chemistry - A European Journal,
Journal Year:
2024,
Volume and Issue:
30(59)
Published: Aug. 12, 2024
An
efficient
approach
for
the
synthesis
of
substituted
aryl
naphthoquinones
via
a
Pd(II)-catalyzed
template-assisted
m-C(sp
Language: Английский