Molecules,
Journal Year:
2023,
Volume and Issue:
28(9), P. 3851 - 3851
Published: May 1, 2023
Despite
extensive
research
in
the
field
of
thrombotic
diseases,
prevention
blood
clots
remains
an
important
area
study.
Therefore,
development
new
anticoagulant
drugs
with
better
therapeutic
profiles
and
fewer
side
effects
to
combat
thrombus
formation
is
still
needed.
Herein,
we
report
synthesis
evaluation
novel
pyrroloquinolinedione-based
rhodanine
derivatives,
which
were
chosen
from
24
developed
derivatives
by
docking
as
potential
molecules
inhibit
clotting
factors
Xa
XIa.
For
hybrid
pyrrolo[3,2,1-ij]quinoline-2-one,
used
a
convenient
structural
modification
tetrahydroquinoline
fragment
varying
substituents
positions
2,
4,
6.
In
addition,
design
target
was
achieved
alkylating
amino
group
propargyl
bromide
or
replacing
2-thioxoimidazolidin-4-one.
The
vitro
testing
showed
that
eight
are
capable
inhibiting
both
coagulation
factors,
two
compounds
selective
inhibitors
factor
Xa,
Overall,
these
data
indicate
activity
through
inhibition
Scientific Reports,
Journal Year:
2022,
Volume and Issue:
12(1)
Published: Oct. 10, 2022
Abstract
Two
new
classes
of
hybrid
quinoline–imidazole/benzimidazole
derivatives
(the
QIBS
salts
and
QIBC
cycloadducts)
were
designed
synthesized
to
evaluate
their
anticancer
antimicrobial
activity.
The
strategy
adopted
for
synthesis
is
straight
efficient,
in
four
steps:
N
-acylation,
-alkylation,
quaternization
a
Huisgen
3
+
2
cycloaddition.
vitro
single-dose
assay
forty
six
quinoline-benzimidazole
compounds
reveal
that
one
salt
(
11h
),
has
an
excellent
quasi
nonselective
activity
against
all
type
cancer
cell
with
PGI
the
area
90–100%
very
good
lethality.
Three
others
hybrids
8h
,
12h
12f
)
selective
some
lines:
breast
MDA-MB-468
Leukemia
HL-60
TB).
five-dose
screening
confirms
compound
possesses
anti-proliferative
activity,
GI
50
range
nano
-molar,
TB,
K-526,
RPMI-8226,
Breast
MDA-MB-468,
Lung
HOP-92
Ovarian
IGROV1.
antibacterial
indicates
three
12c
12d
have
Gram-negative
bacteria
E.
coli
(superior
control
Gentamicin)
while
Gram-positive
S.
aureus
only
8i
(R
=
-CF3)
exhibits
significant
Gentamicin).
MIC
two
other
are
biologically
active
low
concentration,
-molar.
We
believe
these
assets
related
activities,
make
from
our
bearing
phenyl
group
–C
6
H
5
para
(4)-position
benzoyl
moiety
candidate
future
drug
developing.
Molecules,
Journal Year:
2022,
Volume and Issue:
27(19), P. 6632 - 6632
Published: Oct. 6, 2022
Cancer
is
one
of
the
top
leading
causes
death
worldwide.
It
a
heterogenous
disease
characterized
by
unregulated
cell
proliferation
and
invasiveness
abnormal
cells.
For
treatment
cancer,
natural
products
have
been
widely
used
as
source
therapeutic
ingredients
since
ancient
times.
Although
compounds
their
derivatives
demonstrated
strong
antitumor
activity
in
many
types
poor
pharmacokinetic
properties,
low
selectivity,
limited
bioavailability
restricted
efficacy
against
drug-resistant
cancer
cells
hinder
wide
clinical
application.
Conjugation
with
other
bioactive
molecules
has
given
rise
to
new
field
drug
discovery
resulting
development
novel,
bifunctional
more
potent
drugs
for
therapy
overcome
current
drawbacks.
This
review
discusses
multiple
categories
such
conjugates
highlights
recent
trends
advances
product
hybrids.
Among
them,
ADCs,
PDCs,
ApDCs,
PROTACs
AUTOTACs
represent
emerging
agents
cancer.
Asian Journal of Organic Chemistry,
Journal Year:
2024,
Volume and Issue:
13(5)
Published: Feb. 16, 2024
Abstract
Fused
quinolines
have
gained
substantial
attention
due
to
their
significant
biological
and
wide‐spectrum
synthetic
applications.
This
review
supplies
an
encyclopedic
document
regarding
the
approaches
developed
for
synthesis
of
fused‐cyclic
based
on
ring
volume
size
reported
thus
far.
collected
information
will
be
valuable
medicinal
chemists
obtain
knowledge
designing
new
in
order
access
active
compounds.
ChemistrySelect,
Journal Year:
2024,
Volume and Issue:
9(1)
Published: Jan. 7, 2024
Abstract
We
have
presented
the
synthesis
of
some
new
quinoline
linked
fused
isoxazoles
via
copper
(I)
catalyzed
azide
alkyne
cycloaddition
(CuAAC)
followed
by
intramolecular
C−H
arylation
isoxazole
ring
using
PdCl
2
(PPh
3
)
catalyst.
All
synthesized
compounds
were
investigated
for
anticancer
activity
against
three
human
breast
cancer
cell
lines
such
as
MCF‐7,
MDA‐MB‐468
and
MDA‐MB‐231
MTT
assay
5‐fluorouracil
(5‐FU)
was
used
a
standard
drug.
In
this
study,
exhibited
greater
than
reference
drug
5‐FU
which
further
screened
in
vitro
tyrosine
kinase
EGFR
inhibition
molecular
docking
studies
taking
protein
target.
Finally,
insilico
pharmacokinetic
profile
same
obtained
SWISSADME
where
two
following
Lipinski,
Ghose,
Veber,
Egan,
Muegge
rules.
RSC Advances,
Journal Year:
2024,
Volume and Issue:
14(10), P. 7006 - 7021
Published: Jan. 1, 2024
The
demand
for
a
wide
array
of
functional
chemicals
and
materials
has
experienced
significant
surge
in
tandem
with
the
advancement
civilization.
Regrettably,
number
perilous
solvents
are
employed
chemical
laboratories
industrial
settings,
posing
risks
to
well-being
researchers
contributing
environmental
degradation
through
pollution.
Eutectogels,
which
based
on
eutectic
concept,
may
be
synthesized
by
self-assembling
or
self-polymerization
various
components
when
put
under
UV
irradiation
(254
nm).
A
novel
copolymeric
deep
solvent
(DES)
was
successfully
synthesized,
comprising
choline
chloride
(HBA)
as
hydrogen
bond
acceptor,
acetamide
(HBD)
donor,
tetraethyl
orthosilicate
(TEOS),
formic
acid.
In
this
study,
we
present
preparation
four-component
ETGs
synthesizing
pyridine
chromene
derivatives
reusable
catalyst
multi-component
pathway
without
solvents.
procedure
these
heterocyclic
compounds
is
free
using
toxic
it
could
categorized
green
method.
