ChemistrySelect,
Journal Year:
2024,
Volume and Issue:
9(8)
Published: Feb. 22, 2024
Abstract
Design
of
spirocyclic
scaffolds,
which
are
able
for
direct
interaction
with
biological
targets,
is
a
developing
trend
in
medicinal
chemistry.
In
continuation
the
previous
work
on
HIV‐1
inhibitors,
synthetic
approach
towards
spiro[imidazole‐4,3′‐pyrrolo[1,2‐a]quinolin]‐5‐ones
via
1,3‐dipolar
cycloaddition
quinolinium
ylides
arylydeneimidazol‐4‐ones
was
outlined.
Derivatives
various
substitution
pattern
were
prepared
42–86
%
yields.
Use
2,2,2‐trifluoroethanol
as
solvent
crucial
successful
preparation
derivatives,
its
role
sought
prolonging
lifetime
cycloadducts.
RSC Advances,
Journal Year:
2023,
Volume and Issue:
13(47), P. 32858 - 32892
Published: Jan. 1, 2023
This
review
highlights
recent
developments
in
the
microwave-assisted
organic
synthesis
of
N-
and
O-containing
heterocycles
with
specific
examples
pyrazolopyrimidines-,
coumarin-,
quinoline-,
isatin-based
scaffolds
their
associated
biological
activities.
RSC Advances,
Journal Year:
2024,
Volume and Issue:
14(9), P. 5690 - 5728
Published: Jan. 1, 2024
VEGF,
an
important
category
of
tyrosine
kinases,
and
its
receptors
(VEGFR)
are
hyper-activated
in
different
cancers.
The
recently
reported
indolyl
analogs
with
potential
antineoplastic
VEGFR
inhibitory
properties
highlighted.
Molecules,
Journal Year:
2023,
Volume and Issue:
28(12), P. 4817 - 4817
Published: June 16, 2023
Leishmaniasis
is
a
neglected
tropical
disease,
and
there
an
emerging
need
for
the
development
of
effective
drugs
to
treat
it.
To
identify
novel
compounds
with
antileishmanial
properties,
series
functionalized
spiro[indoline-3,2'-pyrrolidin]-2-one/spiro[indoline-3,3'-pyrrolizin]-2-one
23a-f,
24a-f,
25a-g
were
prepared
from
natural-product-inspired
pharmaceutically
privileged
bioactive
sub-structures,
i.e.,
isatins
20a-h,
various
substituted
chalcones
21a-f,
22a-c
amino
acids,
via
1,3-dipolar
cycloaddition
reactions
in
MeOH
at
80
°C
using
microwave-assisted
approach.
Compared
traditional
methods,
synthesis
produces
higher
yields
better
quality,
it
takes
less
time.
We
report
here
vitro
activity
against
Leishmania
donovani
SAR
studies.
The
analogues
24a,
24e,
24f,
25d
found
be
most
active
showed
IC50
values
2.43
µM,
0.96
1.62
3.55
respectively,
compared
standard
reference
drug
Amphotericin
B
(IC50
=
0.060
µM).
All
assessed
DNA
topoisomerase
type
IB
inhibition
Camptothecin,
potential
results.
In
order
further
validate
experimental
results
gain
deeper
understanding
binding
manner
such
compounds,
molecular
docking
studies
also
performed.
stereochemistry
spirooxindole
derivatives
was
confirmed
by
single-crystal
X-ray
crystallography
RSC Advances,
Journal Year:
2024,
Volume and Issue:
14(12), P. 8481 - 8501
Published: Jan. 1, 2024
1,3-Dipolar
cycloaddition
is
one
of
the
important
chemical
reactions
between
a
1,3-dipole
and
dipolarophile
to
construct
five-membered
heterocyclic
compound.
As
an
available
α-amino
acid
reactant,
l-proline
extensively
used
in
1,3-dipolar
reactions.
A
diverse
spectrum
bioactive
spiro
fused
N-heterocycles
obtained
through
this
synthetic
approach.
In
review,
we
have
described
use
synthesis
various
spiro-
scaffolds.
Cyclic
peptides
are
highly
valued
synthetic
targets
in
organic
and
medicinal
chemistry.
The
development
of
new
methodologies
for
peptide
macrocyclization,
different
from
classical
lactamization,
is
essential
the
progress
field.
Herein,
we
report
an
efficient
diastereoselective
macrocyclization
strategy
synthesis
cyclic
using
1,3-dipolar
cycloaddition
azomethine
ylides.
Linear
precursors
length
bearing
diverse
amino
acids
have
shown
to
be
compatible
with
this
method
(26
examples),
giving
good
yields
almost
complete
diastereoselectivity.
DFT
calculations
suggest
a
stepwise
mechanism
which
Cu
plays
key
role
reagents
preorganization.
ChemistrySelect,
Journal Year:
2024,
Volume and Issue:
9(28)
Published: July 24, 2024
Abstract
A
catalyst‐free,
one‐pot
1,3‐dipolar
cycloaddition
reaction
between
azomethine
ylides
(generated
in
situ)
and
(
E
)‐3‐styrylquinoxalin‐2(1
H
)‐ones
led
to
the
formation
of
a
series
quinoxalinone
containing
spiropyrrolidine‐oxindoles.
Subsequently,
vitro
cytotoxicity
synthesized
derivatives
against
panel
Human
NCI‐60
cancer
cell
lines
alongside
normal
was
evaluated
using
SRB
assay.
Among
all
derivatives,
4
h
found
be
most
potent,
selective,
restrict
migration
induce
apoptosis
with
elevated
ROS
levels
HCT‐116.
This
study
emphasizes
potency
as
promising
leads
for
further
development
potent
anti‐cancer
agents.
