Future Medicinal Chemistry,
Journal Year:
2025,
Volume and Issue:
unknown, P. 1 - 17
Published: March 30, 2025
Lung
cancer
has
become
the
most
prevalent
for
past
three
decades,
and
5-years
survival
rate
of
lung
is
only
~20%
nowadays.
Chemotherapy
mainstay
therapy,
especially
non-small
cell
cancer.
However,
drug
resistance
represents
a
principal
cause
therapeutic
failure
in
leading
to
insensitivity,
tumor
recurrence,
disease
progression.
Indole
hybrids
have
potential
conquer
resistance,
enhance
efficacy,
reduce
adverse
events,
improve
pharmacokinetic
properties
due
their
capacity
inhibit
multiple
targets
simultaneously.
Moreover,
indole
osimertinib,
mobocertinib,
cediranib,
vizimpro
are
currently
applied
clinics
demonstrating
that
valuable
scaffolds
treatment
eradication
This
review
provides
comprehensive
overview
evolving
landscape
with
vitro
vivo
efficacy
against
cancer,
structure–activity
relationships
as
well
mechanisms
action
also
discussed,
covering
articles
published
from
2021
onward.
Chemical Reviews,
Journal Year:
2023,
Volume and Issue:
123(4), P. 1364 - 1416
Published: Jan. 17, 2023
Hypervalent
aryliodoumiums
are
intensively
investigated
as
arylating
agents.
They
excellent
surrogates
to
aryl
halides,
and
moreover
they
exhibit
better
reactivity,
which
allows
the
corresponding
arylation
reactions
be
performed
under
mild
conditions.
In
past
decades,
acyclic
aryliodoniums
widely
explored
However,
unmet
need
for
is
improvement
of
their
notoriously
low
reaction
economy
because
coproduced
iodides
during
often
wasted.
Cyclic
have
intrinsic
advantage
in
terms
economy,
started
receive
considerable
attention
due
valuable
synthetic
applications
initiate
cascade
reactions,
can
enable
construction
complex
structures,
including
polycycles
with
potential
pharmaceutical
functional
properties.
Here,
we
summarizing
recent
advances
made
research
field
cyclic
aryliodoniums,
nascent
design
aryliodonium
species
applications.
First,
general
preparation
typical
diphenyl
iodoniums
described,
followed
by
heterocyclic
monoaryl
iodoniums.
Then,
initiated
arylations
coupled
subsequent
domino
summarized
construct
polycycles.
Meanwhile,
building
biaryls
axial
atropisomers
discussed
a
systematic
manner.
Finally,
very
advance
employed
halogen-bonding
organocatalysts
described.
ChemistrySelect,
Journal Year:
2023,
Volume and Issue:
8(1)
Published: Jan. 2, 2023
Abstract
Heterocycles
are
a
privileged
motif
that
appears
as
momentous
objective
in
medicinal
chemistry.
An
important
class
of
compounds
for
drug
discovery
and
design
is
indole
its
derivatives,
which
have
been
examined
variety
biological
activities.
Therefore,
it
noteworthy
the
modern
progress
synthetic,
chemistry;
last
decade
has
onlooker
with
multitude
reports
on
several
derivatives
corroborating
these
chemical
entities
to
be
renowned
target
new
drugs.
The
current
study
includes
brief
natural
sources
indole,
range
commercially
available
indole‐based
Additionally,
this
review
discusses
numerous
facets
structure‐activity
relationship
(SARs)
provides
information
about
varied
pharmacological
effects
derivatives.
literature
data
presented
anti‐pharmacological
agents
herein
covers
largely
from
year
2015
mid
2022.
ACS Omega,
Journal Year:
2023,
Volume and Issue:
8(7), P. 6968 - 6981
Published: Feb. 8, 2023
The
structure-based
design
introduced
indoles
as
an
essential
motif
in
designing
new
selective
estrogen
receptor
modulators
employed
for
treating
breast
cancer.
Therefore,
here,
a
series
of
synthesized
vanillin-substituted
indolin-2-ones
were
screened
against
the
NCI-60
cancer
cell
panel
followed
by
vivo,
vitro,
and
silico
studies.
Physicochemical
parameters
evaluated
with
HPLC
SwissADME
tools.
compounds
demonstrated
promising
anti-cancer
activity
MCF-7
line
(GI
=
6-63%).
compound
highest
(6j)
was
(IC50
17.01
μM)
no
effect
on
MCF-12A
normal
supported
real-time
analysis.
A
morphological
examination
used
lines
confirmed
cytostatic
6j.
It
inhibited
both
vivo
vitro
estrogenic
activity,
triggering
38%
reduction
uterine
weight
induced
immature
rat
model
hindering
62%
ER-α
receptors
settings.
In
molecular
docking
dynamics
simulation
studies
stability
6j
protein-ligand
complex.
Herein,
we
report
that
indolin-2-one
derivative
is
lead
further
pharmaceutical
formulations
potential
anti-breast
drug.
Archiv der Pharmazie,
Journal Year:
2022,
Volume and Issue:
355(6)
Published: April 6, 2022
Abstract
Cancer,
characterized
by
a
deregulation
of
the
cell
cycle
which
mainly
results
in
progressive
loss
cellular
differentiation
and
uncontrolled
growth,
remains
prominent
cause
death
across
world.
Almost
all
currently
available
anticancer
agents
used
clinical
practice
have
developed
multidrug
resistance,
creating
an
urgent
need
to
develop
novel
chemotherapeutics.
Benzimidazole
derivatives
could
exert
properties
through
diverse
mechanisms,
inclusive
disruption
microtubule
polymerization,
induction
apoptosis,
(G2/M)
arrest,
antiangiogenesis,
blockage
glucose
transport.
Moreover,
several
benzimidazole‐based
already
been
approved
for
treatment
cancers.
Hence,
benzimidazole
are
useful
scaffolds
development
agents.
In
particular,
hybrids
dual
or
multiple
antiproliferative
activities
had
potential
overcome
drug
demonstrating
as
prototypes
deployment
control
eradication
The
purpose
present
review
article
is
provide
comprehensive
landscape
agents,
structure–activity
relationship
well
mechanisms
action
also
discussed
facilitate
further
rational
design
more
effective
candidates,
covering
articles
published
from
2019
2021.
Anti-Cancer Agents in Medicinal Chemistry,
Journal Year:
2022,
Volume and Issue:
22(19), P. 3196 - 3207
Published: April 5, 2022
Abstract:
Cancer,
a
crucial
global
health
problem,
is
characterized
by
abnormal
cell
division
and
uncontrolled
growth.
According
to
WHO,
cancer
the
second
leading
cause
of
deaths
accounted
for
approximately
9.6
million
or
one
in
six
2018.
The
National
Cancer
Registry
Programme
Report
2020,
released
ICMRIndia,
estimated
that
there
would
be
13,90,000
cases
India
2020
this
number
likely
rise
15,70,000
2025.
In
spite
several
anti-cancer
drugs,
cannot
cured
completely,
especially
at
late
stages.
current
era,
almost
every
person
suffering
from
some
kind
disease.
Thus,
it
necessity
time
develop
novel,
potent
bioactive
molecules.
Many
researchers
are
working
on
development
new
lead
molecules
finding
biological
target
betterment
human
beings.
However,
heterocycles
constantly
being
used
discovery
clinically
approved
drugs
contain
heterocyclic
core
as
these
show
exhilarating
pharmaceutical
properties,
including
agents
such
methotrexate,
vinblastine,
vincristine,
daunorubicin,
5-fluorouracil,
doxorubicin,
etc.
compounds
provide
fascinating
research
area
design
drug(s).
Herein,
we
focused
natural
well
synthetic
compounds.
Furthermore,
efforts
have
been
made
toward
mechanism
action
selected
