Chemistry & Biodiversity,
Journal Year:
2024,
Volume and Issue:
21(12)
Published: Aug. 23, 2024
Abstract
Chalcone‐incorporated
pyridine‐pyrimidines
i.e.
derivatives
of
(5‐(6‐(pyrimidin‐5‐yl)pyridin‐3‐yl)thiophen‐2‐yl)prop‐2‐en‐1‐one
were
synthesized
and
their
structures
confirmed
by
analytical
techniques.
In
addition,
all
the
examined
for
capacity
to
fight
against
cancer
towards
four
cell
lines,
including
breast
(MCF‐7),
prostate
(DU‐145
PC3),
lung
(A549)
utilizing
MTT
technique
clinically
used
chemotherapy
medication,
etoposide
serving
as
a
positive
reference.
All
these
results
expressed
in
IC
50
μM,
values
compounds
are
compared
with
reference
drug,
showing
ranging
from
1.97±0.45
μM
3.08±0.135
μM.
Among
those,
few
10(a–e
)
demonstrated
strong
activities
corresponding
lines.
Egyptian Journal of Chemistry,
Journal Year:
2023,
Volume and Issue:
0(0), P. 0 - 0
Published: May 3, 2023
The
diseases-related
complications
and
causes
are
threaded.Accordingly,
the
preparation
of
one
drug
with
multiple
targets
is
very
pressing.In
this
context,
three
series
pyrazole-based
derivatives
7a-c,
9a-c,
11a-c
were
designed
synthesized
by
using
5-amino-pyrazoles
3a-c
as
starting
materials.The
structures
various
products
characterized
devices
(elemental
analysis
spectral
tools).The
biological
activities
pyrazolebased
estimated
antioxidant,
anti-diabetic,
anti-Alzheimer,
anti-arthritic.The
estimation
results
showed
that
two
7c
11a
displayed
powerful
activities.In
silico
(physicochemical,
drug-likeness,
toxicity
properties)
was
performed.This
research
could
be
valuable
for
exploration
targets.
Crystals,
Journal Year:
2023,
Volume and Issue:
13(6), P. 890 - 890
Published: May 29, 2023
The
pincer
ligand
2,4-bis(3,5-dimethyl-1H-pyrazol-1-yl)-6-methoxy-1,3,5-triazine
(bpmt)
was
used
to
synthesize
the
novel
[Na(bpmt)2][AuCl4]
complex
through
self-assembly
method.
In
this
complex,
Na(I)
ion
is
hexa-coordinated
with
two
tridentate
N-pincer
ligands
(bpmt).
bpmt
units
are
meridionally
coordinated
via
one
short
Na-N(s-triazine)
and
slightly
longer
Na-N(pyrazole)
bonds,
resulting
in
a
distorted
octahedral
geometry
around
ion.
ligand,
s-triazine
core
not
found
be
coplanar
pyrazole
moieties.
Additionally,
strongly
twisted
from
another
by
64.94°.
Based
on
Hirshfeld
investigations,
H···H
(53.4%)
interactions
have
significant
role
controlling
supramolecular
arrangement
of
complex.
addition,
Cl···H
(12.2%),
C···H
(11.5%),
N···H
(9.3%),
O···H
(4.9%)
significant.
Antimicrobial
investigations
revealed
that
has
promising
antibacterial
antifungal
activities.
showed
enhanced
activity
for
majority
studied
gram-positive
gram-negative
bacteria
compared
free
(MIC
=
62.5–125
µg/mL
vs.
MIC
62.5–500
µg/mL,
respectively)
Amoxicillin
>
500
µg/mL)
as
positive
control.
had
better
efficacy
125
against
C.
albicans
µg/mL).
Archiv der Pharmazie,
Journal Year:
2024,
Volume and Issue:
357(10)
Published: June 29, 2024
Breast
cancer
stands
as
the
leading
cause
of
cancer-related
deaths
among
women
globally,
but
current
therapy
is
restricted
to
serious
adverse
effects
and
multidrug
resistance,
necessitating
exploration
novel,
safe,
efficient
anti-breast
chemotherapeutic
agents.
Pyrazoles
exhibit
excellent
potential
for
utilization
effective
agents
due
their
ability
act
on
various
biological
targets.
Particularly,
pyrazole
hybrids
demonstrated
advantage
targeting
multiple
pathways,
some
them,
which
are
exemplified
by
larotrectinib
(pyrazolo[1,5-a]pyrimidine
hybrid),
can
be
applied
breast
therapy.
Thus,
hold
great
promise
useful
therapeutic
interventions
cancer.
The
aim
this
review
summarize
scenario
with
in
vitro
and/or
vivo
potential,
along
modes
action
structure-activity
relationships,
covering
articles
published
from
2020
present,
streamline
development
rational,
safe
candidates.
