Future Medicinal Chemistry,
Год журнала:
2024,
Номер
16(11), С. 1087 - 1107
Опубликована: Май 9, 2024
Aim:
Using
molecular
hybridization
approach,
novel
18
quinoline
derivatives
(6a–11)
were
designed
and
synthesized
as
EGFR-TK
inhibitors.
Materials
&
methods:
The
antiproliferative
activity
was
assessed
against
breast
(MCF-7),
leukemia
(HL-60)
lung
(A549)
cancer
cell
lines.
Moreover,
the
most
active
(6d
8b)
further
investigated
for
their
potential
In
addition,
cycle
analysis
apoptosis
induction
conducted.
Results:
A
considerable
cytotoxic
attained
with
IC50
values
spanning
from
0.06
to
1.12
μM.
Besides,
6d
8b
displayed
potent
inhibitory
EFGR
of
0.18
0.08
μM,
respectively.
Conclusion:
Accordingly,
afforded
can
be
used
promising
lead
anticancer
candidates
future
optimization.
The Open Medicinal Chemistry Journal,
Год журнала:
2022,
Номер
16(1)
Опубликована: Апрель 28, 2022
Heterocyclic
compounds
account
for
the
most
prominent
and
diverse
class
of
organic
compounds.
A
significant
number
heterocyclic
have
been
synthesized
up
to
this
point.
are
rapidly
increasing
in
due
extensive
synthetic
research
also
their
utility.
Such
a
wide
range
uses
field
medicinal
chemistry.
Dyestuff,
sanitizers,
corrosion
inhibitors,
antioxidants,
copolymer
synthesis
additional
well-known
applications.
There
always
distinguishing
characteristics
an
efficient
approach
producing
newly
discovered
moieties.
According
prior
research,
more
than
90%
medicines
containing
developed
after
obtainment
thorough
scientific
grasp
biological
system.
It
was
neoteric
developments
that
these
play
vital
role
curative
chemistry,
exert
anticancer,
anti-inflammatory,
antifungal,
antiallergic,
antibacterial,
anti-HIV,
antiviral,
anti-convulsant,
other
activities.
The
present
article
provides
detailed
information
regarding
such
Signal Transduction and Targeted Therapy,
Год журнала:
2022,
Номер
7(1)
Опубликована: Дек. 5, 2022
Abstract
The
outbreak
of
COVID-19
has
become
a
global
crisis,
and
brought
severe
disruptions
to
societies
economies.
Until
now,
effective
therapeutics
against
are
in
high
demand.
Along
with
our
improved
understanding
the
structure,
function,
pathogenic
process
SARS-CoV-2,
many
small
molecules
potential
anti-COVID-19
effects
have
been
developed.
So
far,
several
antiviral
strategies
were
explored.
Besides
directly
inhibition
viral
proteins
such
as
RdRp
M
pro
,
interference
host
enzymes
including
ACE2
proteases,
blocking
relevant
immunoregulatory
pathways
represented
by
JAK/STAT,
BTK,
NF-κB,
NLRP3
pathways,
regarded
feasible
drug
development.
development
treat
achieved
strategies,
computer-aided
lead
compound
design
screening,
natural
product
discovery,
repurposing,
combination
therapy.
Several
representative
remdesivir
paxlovid
proved
or
authorized
emergency
use
countries.
And
candidates
entered
clinical-trial
stage.
Nevertheless,
due
epidemiological
features
variability
issues
it
is
necessary
continue
exploring
novel
COVID-19.
This
review
discusses
current
findings
for
treatment.
Moreover,
their
detailed
mechanism
action,
chemical
structures,
preclinical
clinical
efficacies
discussed.
Antibiotics
are
becoming
gradually
ineffective
due
to
drug
resistance,
leading
greater
difficulty
in
the
treatment
of
infectious
diseases.
Therefore,
development
new
chemical
entities
with
different
mechanisms
action
is
essential
fight
against
resistant
microorganisms.
Various
studies
have
shown
that
quinoline
hydrazide/hydrazone
derivatives
possess
several
biological
activities,
such
as
antimalarial,
antitubercular,
anticancer,
anti-inflammatory,
and
antimicrobial.
Among
these
antibacterial
activity
noteworthy.
The
synthetic
flexibility
ring
has
led
a
wide
range
structurally
diverse
derivatives,
which
can
act
at
various
bacterial
targets
DNA
gyrase,
glucosamine-6-phosphate
synthase,
enoyl
ACP
reductase,
3-ketoacyl
reductase.
This
review
emphasizes
potential
reported
based
on
substitution
ring.
metal-quinoline
complexes
also
discussed.
aim
this
assemble
scrutinize
latest
reports
promising
area
development.
Molecules,
Год журнала:
2021,
Номер
26(16), С. 4872 - 4872
Опубликована: Авг. 11, 2021
Synthetic
heterocyclic
compounds
have
incredible
potential
against
different
diseases;
pyridines,
phenolic
and
the
derivatives
of
azo
moiety
shown
excellent
antimicrobial,
antiviral,
antidiabetic,
anti-melanogenic,
anti-ulcer,
anticancer,
anti-mycobacterial,
anti-inflammatory,
DNA
binding
chemosensing
activities.
In
present
review,
above-mentioned
activities
nitrogen-containing
(pyridines),
hydroxyl
(phenols)
are
discussed
with
reference
to
minimum
inhibitory
concentration
structure-activity
relationship,
which
clearly
indicate
that
presence
nitrogen
in
phenyl
ring;
addition,
substituent
incorporation
a
diazo
group
is
crucial
for
improved
efficacies
probing
diseases.
The
comparison
was
made
reported
drugs
new
synthetic
showed
recent
therapeutic
perspectives
last
five
years.
Molecules,
Год журнала:
2022,
Номер
27(3), С. 1003 - 1003
Опубликована: Фев. 2, 2022
Late-stage
modification
of
drug
molecules
is
a
fast
method
to
introduce
diversity
into
the
already
biologically
active
scaffold.
A
notable
number
analogs
mefloquine,
chloroquine,
and
hydroxychloroquine
have
been
synthesized,
starting
from
readily
available
pharmaceutical
ingredient
(API).
In
current
review,
all
modifications
sites
reactivity
types
are
summarized
provide
insight
chemistry
these
molecules.
The
approaches
include
introduction
simple
groups
functionalities.
Coupling
other
drugs,
polymers,
or
carriers
afforded
hybrid
compounds
conjugates
with
either
easily
hydrolyzable
more
chemically
inert
bonds.
utility
some
was
tested
in
antiprotozoal,
antibacterial,
antiproliferative
assays,
as
well
enantiodifferentiation
experiments.
RSC Advances,
Год журнала:
2025,
Номер
15(1), С. 231 - 243
Опубликована: Янв. 1, 2025
Quinoline-based
dihydrazone
derivative
3b
showed
multiple
anticancer
mechanisms.
could
not
only
induce
apoptosis
of
MCF-7
cells
and
bind
to
DNA
,
but
also
act
as
a
CDK2
inhibitor.
