Abstract
New
benzimidazole‐based
piperazine
analogues
(
9
a
–
n
)
were
synthesized
and
screened
for
their
cytotoxicity
against
human
breast
cancer
cell
lines
MCF‐7
MDA‐MB‐231
by
employing
Doxorubicin
as
standard
reference.
4‐(trifluoromethyl)benzyl
substituted
compound
f
displayed
outstanding
activity
both
line
with
IC
50
value
of
7.29±0.20
μM
6.92±4.80
respectively,
compared
to
.
Additionally,
butyl
m
showed
superior
cells
7.61±5.90
4‐fluorobenzyl
c
indicated
on
par
the
an
9.15±0.10
The
morphological
study
active
compounds
revealed
have
not
shown
any
toxicity
MCF‐10A
cells.
Molecular
docking
all
Cyclin‐dependent
kinase
6
produced
notable
binding
energies
interactions
in
comparison
co‐crystalized
ligand
Abemaciclib
Pharmacokinetic
evaluation
presented
favourable
drug‐likeness
properties.
The Journal of Organic Chemistry,
Год журнала:
2024,
Номер
89(11), С. 7513 - 7520
Опубликована: Май 9, 2024
A
Rh(III)-catalyzed
annulation
of
2-arylbenzimidazoles
with
α-diazo
carbonyl
compounds
via
C–H
activation/carbene
insertion/intramolecular
cyclization
is
explored.
The
switchable
product
selectivity
achieved
by
the
use
distinct
compounds.
Benzimidazole-fused
quinolines
are
obtained
through
[4
+
2]
exclusively
when
2-diazocyclohexane-1,3-diones
used,
where
they
act
as
a
C2
synthon.
Alternatively,
diazonaphthalen-1(2H)-ones
merely
function
one-carbon
unit
synthon
to
generate
quaternary
center
1]
afford
spirocyclic
benzimidazole-fused
isoindole
naphthalen-2-ones.
thorough
mechanistic
study
reveals
course
reaction.
The
N-benzyl
piperidine
(N-BP)
structural
motif
is
commonly
employed
in
drug
discovery
due
to
its
flexibility
and
three-dimensional
nature.
Medicinal
chemists
frequently
utilize
the
N-BP
as
a
versatile
tool
fine-tune
both
efficacy
physicochemical
properties
development.
It
provides
crucial
cation-π
interactions
with
target
protein
also
serves
platform
for
optimizing
stereochemical
aspects
of
potency
toxicity.
This
found
numerous
approved
drugs
clinical/preclinical
candidates.
review
focuses
on
applications
campaigns,
emphasizing
role
imparting
medicinally
relevant
properties.
an
overview
drugs,
clinical
preclinical
pipeline,
discusses
utility
specific
therapeutic
targets
indications,
along
potential
challenges.
In
this
study,
two
new
molecules
were
synthesized
from
the
reaction
of
2-methyl-1H-benzo[d]imidazole
with
aryl
halides
in
presence
a
strong
base.
The
structures
newly
1,2-disubstituted
benzimidazole
compounds
characterized
using
spectroscopic
techniques
(FT-IR,
Anti-Cancer Agents in Medicinal Chemistry,
Год журнала:
2022,
Номер
22(19), С. 3280 - 3290
Опубликована: Апрель 30, 2022
Cancer
is
a
life-threatening
disease.
Anti-cancer
drugs
are
the
focus
of
research.
The
heterocyclic
molecules
like
benzimidazole
occupy
central
position
in
searching
for
novel
and
effective
anti-cancer
drugs.
medicinal
chemists
designed
synthesized
several
derivatives
conjugates
to
evaluate
them
as
potential
agents.The
purpose
this
compilation
literature
cover
progress
benzimidazole-based
agents,
their
synthesis,
evaluation
cancer
disease
treatment.The
recent
literatures
have
been
collected
from
various
search
engines
peer-reviewed
journals.The
compounds
dehydroabietic
acid,
piperidyl
carboxamide,
benzimidazole-quinazolinone
hybrids,
benzimidazole-thiazole
conjugate,
pendant
cyanopyrimidine
discussed
detail.This
review
article
will
help
design
synthesize
agents.
Abstract
New
benzimidazole‐based
piperazine
analogues
(
9
a
–
n
)
were
synthesized
and
screened
for
their
cytotoxicity
against
human
breast
cancer
cell
lines
MCF‐7
MDA‐MB‐231
by
employing
Doxorubicin
as
standard
reference.
4‐(trifluoromethyl)benzyl
substituted
compound
f
displayed
outstanding
activity
both
line
with
IC
50
value
of
7.29±0.20
μM
6.92±4.80
respectively,
compared
to
.
Additionally,
butyl
m
showed
superior
cells
7.61±5.90
4‐fluorobenzyl
c
indicated
on
par
the
an
9.15±0.10
The
morphological
study
active
compounds
revealed
have
not
shown
any
toxicity
MCF‐10A
cells.
Molecular
docking
all
Cyclin‐dependent
kinase
6
produced
notable
binding
energies
interactions
in
comparison
co‐crystalized
ligand
Abemaciclib
Pharmacokinetic
evaluation
presented
favourable
drug‐likeness
properties.
