Current Topics in Medicinal Chemistry,
Journal Year:
2021,
Volume and Issue:
21(8), P. 737 - 752
Published: March 1, 2021
Undoubtedly,
antibiotics
have
saved
billions
of
lives,
but
lack
novel
antibiotics,
development
resistance
mechanisms
in
almost
all
clinical
isolates
bacteria,
and
recurrent
infections
caused
by
persistent
bacteria
hamper
the
successful
treatment
infections.
Due
to
widespread
emergence
resistance,
even
new
families
anti-microbial
agents
a
short
life
expectancy.
Drugs
acting
on
single
target
often
lead
drug
are
associated
with
various
side
effects.
For
overcoming
this
problem,
either
multidrug
therapy,
or
multiple
targets
may
be
used.
The
latter
is
called
‘hybrid
molecules,’
which
formed
clubbing
two
biologically
active
pharmacophores
together,
without
an
appropriate
linker.
In
rapidly
evolving
era,
natural
product-based
hybrid
molecules
super-alternative
for
combating
bacterial
fungal
strains.
Coumarins
(benzopyran-2-one)
one
earliest
reported
plant
secondary
metabolites
having
clinically
proven
diverse
range
pharmacological
properties.
On
other
hand,
1,2,3-triazole
common
pharmacophore
many
drugs
responsible
polar
interactions,
improving
solubility
binding
affinity
biomolecular
targets.
review,
we
discuss
recent
advances
Coumarin-1,2,3-triazole
hybrids
as
potential
anti-bacterial
agents,
aiming
provide
useful
platform
exploration
leads
broader
spectrum,
more
effectiveness
less
toxicity
modes
action
cost-effective
safer
future.
Biomolecules,
Journal Year:
2021,
Volume and Issue:
11(6), P. 894 - 894
Published: June 16, 2021
Chalcones
(1,3-diaryl-2-propen-1-ones)
are
precursors
for
flavonoids
and
isoflavonoids,
which
common
simple
chemical
scaffolds
found
in
many
naturally
occurring
compounds.
Many
chalcone
derivatives
were
also
prepared
due
to
their
convenient
synthesis.
as
weandhetic
analogues
have
attracted
much
interest
broad
biological
activities
with
clinical
potentials
against
various
diseases,
particularly
antitumor
activity.
The
family
has
demonstrated
potential
vitro
vivo
activity
cancers
via
multiple
mechanisms,
including
cell
cycle
disruption,
autophagy
regulation,
apoptosis
induction,
immunomodulatory
inflammatory
mediators.
It
represents
a
promising
strategy
develop
chalcones
novel
anticancer
agents.
In
addition,
the
combination
of
other
therapies
is
expected
be
an
effective
way
improve
therapeutic
efficacy.
However,
despite
encouraging
results
response
observed
studies,
full
description
toxicity
required
use
safe
drugs
treatment
cancer.
this
review,
we
will
summarize
recent
advances
agents
mechanisms
action.
Besides,
future
applications
scope
toward
prevention
cancer
brought
out.
European Journal of Medicinal Chemistry Reports,
Journal Year:
2022,
Volume and Issue:
5, P. 100038 - 100038
Published: March 2, 2022
Coumarin
derivatives
are
important
class
of
natural
plant
metabolites
that
offer
variety
biological
activities.
They
can
also
be
derived
synthetically,
and
a
wide
synthetic
coumarin
(azoles,
sulfonyl,
furan,
pyrazole
etc)
have
shown
promising
anticancer,
antitumor
anti-proliferative
not
only
effective
anticancer
agents,
but
possess
minimum
side
effects.
On
the
basis
different
substitution
patterns,
these
potents
displayed
tremendous
capability
to
regulate
potential
In
view
above,
efforts
been
made
by
scientists
develop
its
scaffolds
minimal
This
review
article
covers
recent
developments
biologically
active
against
various
cancer
cell
lines.
Further,
it
highlights
evaluation
candidates
via
in
vivo,
vitro,
MTT
assay.
The
ongoing
discovery
novel
anti-cancer
agents
their
effectiveness
using
Structural
Activity
Relationship
is
discussed
detail.
RSC Medicinal Chemistry,
Journal Year:
2023,
Volume and Issue:
15(1), P. 10 - 54
Published: Oct. 20, 2023
Many
researchers
around
the
world
are
working
on
development
of
novel
anticancer
drugs
with
different
mechanisms
action.
In
this
case,
coumarin
is
a
highly
promising
pharmacophore
for
drugs.
Besides,
hybridization
moiety
other
pharmacophores
has
emerged
as
potent
breakthrough
in
treatment
cancer
to
decrease
its
side
effects
and
increase
efficiency.
This
review
aims
provide
comprehensive
overview
recent
derivatives
their
application
Herein,
we
highlight
describe
largest
number
research
works
reported
field
from
2015
August
2023,
along
action
structure-activity
relationship
studies,
making
articles
published
topic
date.
Archiv der Pharmazie,
Journal Year:
2020,
Volume and Issue:
353(6)
Published: April 6, 2020
Infections
caused
by
Gram-positive
and
-negative
bacteria
are
one
of
the
foremost
causes
morbidity
mortality
globally.
Antibiotics
mainstay
therapy
for
bacterial
infections,
but
emergence
wide
spread
drug-resistant
pathogens
have
already
become
a
huge
issue
public
healthcare
systems.
The
coumarin
moiety,
which
is
ubiquitous
in
nature,
could
bind
to
B
subunit
DNA
gyrase
inhibit
supercoiling
blocking
ATPase
activity;
hence,
derivatives
possess
potential
antibacterial
activity.
Several
coumarin-containing
hybrids
such
as
coumermycin
A1,
clorobiocin,
novobiocin
been
used
clinical
practice
treatment
various
infections;
thus,
it
conceivable
that
hybridization
moiety
with
other
pharmacophores
may
provide
opportunities
development
novel
antibiotics.
This
review
outlines
advances
recent
5
years
structure-activity
relationships
also
discussed.
Medicinal Research Reviews,
Journal Year:
2020,
Volume and Issue:
40(5), P. 2049 - 2084
Published: June 11, 2020
Abstract
The
continuous
emergency
of
drug‐resistant
cancers
and
the
low
specificity
anticancer
agents
have
been
major
challenges
in
control
treatment
cancer,
making
an
urgent
need
to
develop
novel
with
high
efficacy.
Chalcones,
precursors
flavonoids
isoflavonoids,
exhibit
structural
heterogeneity
can
act
on
various
drug
targets.
Chalcones
which
demonstrated
potential
vitro
vivo
activity
against
both
drug‐susceptible
cancers,
are
useful
templates
for
development
agents.
Hybridization
chalcone
moiety
other
pharmacophores
could
provide
hybrids
overcome
resistance
improve
specificity,
so
it
represents
a
promising
strategy
This
review
emphasizes
development,
mechanisms
action
as
well
structure‐activity
relationships
therapeutic
application
many
recent
10
years.
Archiv der Pharmazie,
Journal Year:
2020,
Volume and Issue:
353(8)
Published: May 8, 2020
Abstract
Cancer
can
invade
or
spread
to
almost
all
parts
of
the
body.
The
increasing
morbidity
and
high
mortality
cancer
create
a
great
demand
for
development
novel
anticancer
drugs.
Coumarin
derivatives
are
ubiquitous
in
nature
readily
interact
with
diverse
enzymes
receptors
cells
via
weak
bond
interactions;
hence,
coumarin
is
highly
privileged
pharmacophore
agents.
This
review
will
focus
on
recent
hybrids
as
potential
agents
covering
articles
published
from
2019
2020.