Pd/NBE-Catalyzed One-Pot Modular Synthesis of Tetrahydro-γ-carbolines
The Journal of Organic Chemistry,
Год журнала:
2025,
Номер
unknown
Опубликована: Апрель 14, 2025
Tetrahydro-γ-carbolines
are
especially
outstanding
fused
heterocyclic
ring
systems
possessing
significant
biological
activities
in
the
central
nervous
system.
Here,
using
commercially
available
NBE
derivatives
(NBEs),
we
report
an
efficient
protocol
for
one-pot
modular
synthesis
of
4-substituted
tetrahydro-γ-carbolines
via
Catellani/aza-Michael
addition
cascade
from
easily
3-iodo-1-tosyl-1H-indole,
aziridines
and
olefins.
This
approach
exhibits
a
wide
substrate
scope,
good
yields,
scalability,
potential
extension
toward
Mebhydroline
analogues.
Язык: Английский
A new computational cross-structure-activity relationship (C-SAR) approach applies to a selective HDAC6 inhibitor dataset for accelerated structure development
Computers in Biology and Medicine,
Год журнала:
2025,
Номер
192, С. 110169 - 110169
Опубликована: Май 1, 2025
Язык: Английский
Reversing TGF-β1-induced fibrotic phenotype in human lung fibroblasts using a PROTAC tool derived from an indoline-based HDAC6 inhibitor
European Journal of Medicinal Chemistry Reports,
Год журнала:
2025,
Номер
unknown, С. 100276 - 100276
Опубликована: Май 1, 2025
Язык: Английский
Unlocking the Potential of Histone Deacetylase Inhibitors in Combatting Age-Related Retinal Degenerative Diseases
Ageing Research Reviews,
Год журнала:
2025,
Номер
unknown, С. 102788 - 102788
Опубликована: Май 1, 2025
Язык: Английский
Spirotetrahydroisoquinoline-Based Histone Deacetylase Inhibitors as New Antifibrotic Agents: Biological Evaluation in Human Fibroblasts from Bronchoalveolar Lavages of Idiopathic Pulmonary Fibrosis Patients
ACS Pharmacology & Translational Science,
Год журнала:
2024,
Номер
8(2), С. 380 - 393
Опубликована: Ноя. 12, 2024
Idiopathic
pulmonary
fibrosis
(IPF)
is
a
rare
interstitial
lung
disease
typified
by
progressive
fibrosing
phenotype.
IPF
has
been
associated
with
aberrant
HDAC
activity,
particularly
HDAC6.
Combining
synthetic
and
modeling
studies,
new
family
of
spirotetrahydroisoquinoline-capped
histone
deacetylase
inhibitors
5a–o
was
developed.
These
analogues
were
prepared
via
the
three-component
Castagnoli–Cushman
reaction
(CCR)
as
key
step.
Structure–activity
relationship
(SAR)
studies
identified
5n
(fibrostat)
preferential
HDAC6
inhibitor
suitable
degree
selectivity
compared
to
HDAC1,
HDAC3,
HDAC5,
HDAC8,
HDAC10,
HDAC11.
able
negatively
modulate
expression
fibrotic
markers,
fibronectin
collagen
1,
in
fibroblasts
derived
from
bronchoalveolar
lavages
patients.
In
another
ex
vivo
human
model,
reduced
affected
1
vimentin,
latter
being
invasiveness.
Finally,
fibrostat
did
not
show
toxicity
rat-perfused
heart
zebrafish
larvae.
Язык: Английский
Generating a Peptide Library Using the Repeats of Amino Acid Scaffolds Created by Sliding the Framework of a 7-mer Human Chemerin Segment and Discovery of Potent Antibacterial and Antimycobacterial Peptides
Sariyah Akhtar,
Mohd Mustkim Ansari,
Rahul Dev Verma
и другие.
Journal of Medicinal Chemistry,
Год журнала:
2024,
Номер
unknown
Опубликована: Дек. 24, 2024
The
quest
for
new
approaches
generating
novel
bioactive
designer
proteins/peptides
has
continued
with
their
success
in
various
biomedical
applications.
Previously,
we
designed
a
14-mer
α-helical
peptide
antimicrobial
and
antimycobacterial
activities
by
employing
tandem
repeat
of
the
7-mer,
"KVLGRLV"
human
chemerin
segment.
Herein,
devised
method
"sliding
framework"
this
segment
to
create
amino
acid
scaffolds
varying
sizes
sequences
explored
design
library
antibacterial
activities.
By
utilizing
2
7
repeats
these
6-residue
scaffolds,
synthesized
30
peptides
10–16
residue
lengths.
Thus,
identified
AMPs
α-helical,
β-sheet,
random
coil
structures,
membrane-destabilizing,
intracellular
modes
action,
9
them
showed
therapeutic
indices
between
100
750.
Three
two
nine
vivo
antitubercular
efficacies
against
Escherichia
coli
ATCC
25922
Mycobacterium
bovis
BCG
infections,
respectively,
mouse
model.
Язык: Английский