Organic Letters,
Journal Year:
2025,
Volume and Issue:
unknown
Published: March 19, 2025
A
nickel-catalyzed
reductive
cross-coupling
of
gem-bromofluorocyclopropanes
with
aryl
bromides
for
the
synthesis
monofluorinated
cyclopropane
derivatives
is
reported.
Different
from
cleavage
route
ring
reported
by
previous
works,
this
catalytic
system
shows
excellent
regioselectivity
control
cyclic
selectivity,
giving
as
major
product.
This
transformation
demonstrates
mild
conditions,
high
efficiency,
a
broad
substrate
scope,
and
good
functional
group
compatibility,
providing
facile
method
diversified
cyclopropane-containing
drugs
bioactive
molecules.
Chemico-Biological Interactions,
Journal Year:
2022,
Volume and Issue:
367, P. 110173 - 110173
Published: Sept. 22, 2022
In
total,
twenty
elements
appear
to
be
essential
for
the
correct
functioning
of
human
body,
half
which
are
metals
and
non-metals.
Among
those
that
currently
considered
normal
biological
four
main
group
elements,
sodium
(Na),
potassium
(K),
magnesium
(Mg),
calcium
(Ca),
six
d-block
transition
metal
manganese
(Mn),
iron
(Fe),
cobalt
(Co),
copper
(Cu),
zinc
(Zn)
molybdenum
(Mo).
Cells
have
developed
various
metallo-regulatory
mechanisms
maintaining
a
necessary
homeostasis
metal-ions
diverse
cellular
processes,
most
importantly
in
central
nervous
system.
Since
redox
active
(for
example
Fe
Cu)
may
participate
electron
transfer
reactions,
their
must
carefully
controlled.
The
catalytic
behaviour
escaped
control,
e.g.
via
Fenton
reaction,
results
formation
reactive
hydroxyl
radicals,
cause
damage
DNA,
proteins
membranes.
Transition
integral
parts
centers
numerous
enzymes
(e.g.
Cu,Zn-SOD,
Mn-SOD,
Catalase)
catalyze
chemical
reactions
at
physiologically
compatible
rates.
Either
deficiency,
or
an
excess
result
disease
states
arising
organism.
Some
typical
ailments
characterized
by
disturbed
include
neurological
disorders
(Alzheimer's,
Parkinson's
Huntington's
disorders),
mental
health
problems,
cardiovascular
diseases,
cancer,
diabetes.
To
comprehend
more
deeply
metals,
acting
either
alone
combination,
and/or
through
interaction
with
non-essential
chromium)
function
systems
will
require
application
broader,
interdisciplinary
approach
than
has
mainly
been
used
so
far.
It
is
clear
stronger
cooperation
between
bioinorganic
chemists
biophysicists
-
who
already
achieved
great
success
understanding
structure
role
metalloenzymes
living
biologists,
access
new
avenues
research
biology
ions.
With
this
mind,
present
paper
reviews
selected
aspects
ions
possible
interactions
under
pathological
conditions.
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.
Pharmaceuticals,
Journal Year:
2024,
Volume and Issue:
17(3), P. 281 - 281
Published: Feb. 22, 2024
The
fluorine
atom
possesses
many
intrinsic
properties
that
can
be
beneficial
when
incorporated
into
small
molecules.
These
include
the
atom’s
size,
electronegativity,
and
ability
to
block
metabolic
oxidation
sites.
Substituents
feature
fluorine-containing
groups
are
currently
prevalent
in
drugs
lower
cholesterol,
relieve
asthma,
treat
anxiety
disorders,
as
well
improve
chemical
of
various
medications
imaging
agents.
dye
scaffolds
(fluorescein/rhodamine,
coumarin,
BODIPY,
carbocyanine,
squaraine
dyes)
reported
will
address
incorporation
scaffold
contribution
it
provides
its
application
an
agent.
It
is
also
important
recognize
radiolabeled
atoms
used
for
PET
early
detection
diseases.
This
review
discuss
benefits
incorporating
molecules
give
examples
fluorinated
pharmaceutical
industry
techniques.
Archiv der Pharmazie,
Journal Year:
2025,
Volume and Issue:
358(1)
Published: Jan. 1, 2025
Abstract
Macrocycles
or
medium‐sized
rings
offer
diverse
functionality
and
stereochemical
complexity
in
a
well‐organized
ring
structure,
allowing
them
to
fulfill
various
biochemical
functions,
resulting
high
affinity
selectivity
for
protein
targets,
while
preserving
sufficient
bioavailability
reach
intracellular
compartments.
These
features
have
made
macrocycles
attractive
candidates
organic
synthesis
drug
discovery.
Since
the
20th
century,
more
than
three‐score
macrocyclic
drugs,
including
radiopharmaceuticals,
been
approved
by
US
Food
Drug
Administration
(FDA)
treating
bacterial
viral
infections,
cancer,
obesity,
immunosuppression,
inflammatory,
neurological
disorders,
managing
cardiovascular
diseases,
diabetes,
more.
This
review
presents
17
FDA‐approved
drugs
during
past
5
years,
highlighting
their
importance
critical
role
modern
therapeutics,
innovative
synthetic
approaches
construction
of
these
macrocycles.
Molecules,
Journal Year:
2023,
Volume and Issue:
28(14), P. 5359 - 5359
Published: July 12, 2023
The
altered
activation
or
overexpression
of
protein
kinases
(PKs)
is
a
major
subject
research
in
oncology
and
their
inhibition
using
small
molecules,
inhibitors
(PKI)
the
best
available
option
for
cure
cancer.
pyrazole
ring
extensively
employed
field
medicinal
chemistry
drug
development
strategies,
playing
vital
role
as
fundamental
framework
structure
various
PKIs.
This
scaffold
holds
importance
considered
privileged
based
on
its
synthetic
accessibility,
drug-like
properties,
versatile
bioisosteric
replacement
function.
It
has
proven
to
play
key
many
PKI,
such
Akt,
Aurora
kinases,
MAPK,
B-raf,
JAK,
Bcr-Abl,
c-Met,
PDGFR,
FGFRT,
RET.
Of
74
molecule
PKI
approved
by
US
FDA,
8
contain
ring:
Avapritinib,
Asciminib,
Crizotinib,
Encorafenib,
Erdafitinib,
Pralsetinib,
Pirtobrutinib,
Ruxolitinib.
focus
this
review
unfused
within
clinically
tested
additional
required
elements
chemical
structures.
Related
important
fused
scaffolds
like
indazole,
pyrrolo[1,2-b]pyrazole,
pyrazolo[4,3-b]pyridine,
pyrazolo[1,5-a]pyrimidine,
pyrazolo[3,4-d]pyrimidine
are
beyond
work.
Molecules,
Journal Year:
2023,
Volume and Issue:
28(9), P. 3651 - 3651
Published: April 22, 2023
The
strategic
fluorination
of
oxidatively
vulnerable
sites
in
bioactive
compounds
is
a
relatively
recent,
widely
used
approach
allowing
us
to
modulate
the
stability,
bio-absorption,
and
overall
efficiency
pharmaceutical
drugs.
On
other
hand,
natural
tailor-made
amino
acids
are
traditionally
as
basic
scaffolds
for
development
molecules.
main
goal
this
review
article
emphasize
these
general
trends
featured
recently
approved
ACS Catalysis,
Journal Year:
2025,
Volume and Issue:
unknown, P. 976 - 981
Published: Jan. 1, 2025
Triethoxysilane
was
found
to
be
an
efficient
catalyst
for
the
synthesis
of
E-alkenyl-
and
alkyl-di-boronate
esters
by
single
sequential
hydroboration
terminal
alkynes,
respectively,
with
pinacolborane.
Mechanistic
studies
support
that
formation
diboronate
proceeds
a
double
pathway
steric
electronic
profile
at
Si
being
key
enabling
second
step.
Weak
non-covalent
interactions
involving
C≡C
or
C═C
bonds
in
alkynes
alkenylboronate
have
been
identified
as
responsible
substrate
activation
toward
addition
HBPin.
