Microwave assisted one-pot synthesis of novel 1,3,4-oxadiazole-imidazo[1',5':1,2]pyrrolo[3,4-d][1,2,3]triazoles as potent EGFR targeting Anticancer agents
Опубликована: Янв. 1, 2025
Язык: Английский
Microwave-assisted one-pot synthesis of fused isoxazolo[4′,5′:3,4]pyrrolo[1,2-c]pyrimidines as potent anticancer agents: In vitro and in silico study
Tetrahedron Letters,
Год журнала:
2025,
Номер
162, С. 155570 - 155570
Опубликована: Апрель 8, 2025
Язык: Английский
Synthesis and Anticancer Activity of Isoquinoline‐Imidazo[1,2‐a]Pyridine Linked Sulfonyl Derivatives
ChemistrySelect,
Год журнала:
2025,
Номер
10(15)
Опубликована: Апрель 1, 2025
Abstract
Several
novel
imidazo[1,2‐
a
]pyridine‐isoquinoline‐linked
sulfonyl
derivatives
were
designed
and
synthesized
in
this
study.
These
subsequently
assessed
vitro
for
their
inhibitory
effects
on
EGFR
kinases
antiproliferative
activity
against
two
breast
cancer
cell
lines.
of
the
compounds
demonstrated
satisfactory
efficacy
comparison
to
primary
agent,
erlotinib.
The
most
promising
compounds,
6‐methoxy‐2‐methyl‐1‐(2‐phenyl‐6‐(1‐((3‐(trifluoromethyl)phenyl)sulfonyl)‐1,2,3,6‐tetrahydro
pyridin‐4‐yl)imidazo[1,2‐a]pyridin‐3‐yl)‐1,2,3,4‐tetrahydro
isoquinoline,
6‐methoxy‐2‐methyl‐1‐(2‐phenyl‐6‐(1‐((4‐(trifluoromethoxy)
phenyl)
sulfonyl)‐1,2,3,6‐tetrahydropyridin‐4‐yl)imidazo[1,2‐a]pyridin‐3‐yl)‐1,2,3,4‐tetrahydroisoquinoline,
6‐methoxy‐2‐methyl‐1‐(2‐phenyl‐6‐(1‐((3‐(trifluoromethoxy)phenyl)sulfonyl)‐1,2,3,6‐tetrahydropyridin‐4‐yl)
imidazo[1,2‐a]pyridin‐3‐yl)‐1,2,3,4‐tetrahydroisoquinoline,
exhibited
exceptional
anticancer
MCF‐7
MDA‐MB‐231
lines,
with
IC
50
values
ranging
from
2.69
±
0.24
7.64
0.15
µM.
Subsequently
results
that
above
potent
more
efficacious
than
conventional
medicine
molecular
interactions
human
epidermal
growth
factor
receptor
(EGFR)
(PDB:
4HJO),
which
included
co‐crystallized
ligand
(erlotinib)
evaluated
through
silico
docking
studies.
It
was
noted
binding
energies
all
higher
those
standard
drug,
Язык: Английский
Design and Synthesis of Novel Quinoxaline-Piperazine Linked Isoxazole Conjugates: Anti-cancer Assessment, tyrosine kinase EGFR inhibitory activity, Molecular Docking and DFT Studies
Journal of Molecular Structure,
Год журнала:
2024,
Номер
1321, С. 139839 - 139839
Опубликована: Сен. 6, 2024
Язык: Английский
Halogen‐based quinazolin‐4(3H)‐one derivatives as MCF‐7 breast cancer inhibitors: Current developments and structure–activity relationship
Archiv der Pharmazie,
Год журнала:
2024,
Номер
358(1)
Опубликована: Ноя. 13, 2024
Abstract
Currently,
cancer
is
a
serious
health
challenge
with
predominance
beyond
restrictions.
Breast
remains
one
of
the
major
contributors
to
cancer‐related
morbidity
and
mortality
in
women.
Chemotherapy
continues
be
crucial
treatment
all
variants
cancer.
Several
antitumor
drugs
are
presently
different
phases
clinical
trials,
whereas
many
more
have
been
approved
for
use.
However,
these
potential
cause
adverse
effects,
certain
individuals
may
become
resistant
them,
which
would
eventually
reduce
drug's
efficacy.
Therefore,
it
essential
discover,
develop,
improve
newer
anticancer
drug
molecules
that
could
potentially
inhibit
proliferative
pathways.
In
recent
years,
quinazolinone
derivatives,
specifically
halogen‐substituted
4(3
H
)‐quinazolinone,
drawn
attention
as
promising
new
class
chemotherapeutic
agents.
addition,
showed
significant
inhibition
micromolar
ranges
when
tested
vitro
against
MCF‐7
cell
line.
this
study
aims
emphasize
intriguing
versatility
halogen
atoms,
providing
an
in‐depth
summary
highlighting
developments
properties
halogenated
)‐quinazolinones.
It
also
features
detailed
discussion
structure–activity
relationship
(SAR)
various
functional
groups
their
interaction
amino
acid
residues
utilizing
molecular
docking
studies.
The
intent
foster
novel
discoveries
can
inspire
innovative
investigations
domain.
Hence,
simplifies
design
development
strategies
by
prolonging
array
pharmacologically
active
candidates.
Язык: Английский
The current landscape of 1,2,3‐triazole‐(fused) six‐membered nitrogen‐containing heteroaromatic ring hybrids with anticancer therapeutic potential
Archiv der Pharmazie,
Год журнала:
2024,
Номер
358(1)
Опубликована: Дек. 30, 2024
Cancer,
characterized
by
uncontrolled
growth
and
spread
of
abnormal
cells
potentially
influencing
almost
all
tissues
in
the
body,
is
one
most
devastating
lethal
diseases
throughout
world.
Chemotherapy
principal
approaches
for
cancer
treatment,
but
multidrug
resistance
severe
side
effects
represent
main
barriers
to
success
therapy,
creating
a
vital
need
develop
novel
chemotherapeutic
agents.
The
1,2,3-triazole
moiety
can
be
conveniently
constructed
"click
chemistry"
could
exert
diverse
noncovalent
interactions
with
various
enzymes
cells.
Hence,
fascinating
anticancer
pharmacophores.
Moreover,
also
serve
as
powerful
ligation
tool
complex
molecular
architectures
increase
efficacy
lead
molecules.
Notably,
1,2,3-triazole-containing
hybrids
intriguing
structural
variations
target
different
biological
components
simultaneously,
highlighting
their
potential
treatment
eradication
cancer.
This
review
outlines
current
landscape
1,2,3-triazole-(fused)
six-membered
nitrogen-containing
heteroaromatic
ring
hybrids,
inclusive
1,2,3-triazole-quinazolines,
1,2,3-triazole-quinazolinones,
1,2,3-triazole-quinolines,
1,2,3-triazole-quinolones,
1,2,3-triazole-pyridines,
1,2,3-triazole-pyrimidines,
therapeutic
potential,
explores
mechanisms
action,
critical
aspects
design
well
structure-activity
relationships
(SARs),
covering
articles
published
from
2021
present,
pave
way
development
innovative
efficient
interventions
therapy.
Язык: Английский