Chemical Communications,
Journal Year:
2022,
Volume and Issue:
59(7), P. 868 - 871
Published: Dec. 12, 2022
Macrocycles
often
exhibit
good
biological
properties
and
potential
druggability,
which
lead
to
versatile
applications
in
the
pharmaceutical
industry.
Herein,
we
report
a
highly
efficient
practical
methodology
for
functionalization
macrocyclization
of
Trp
Trp-containing
peptides
via
Pd(II)-catalyzed
C-H
alkenylation
at
C4
position.
This
method
provides
direct
access
maleimide-decorated
peptidomimetics
maleimide-braced
17-
30-membered
peptide
macrocycles.
In
particular,
these
unique
macrocycles
revealed
low
micro-
sub-micromolar
EC50
values
with
promising
anti-SARS-CoV-2
activities.
Further
explorations
computational
methodologies
experimental
validations
indicated
that
exert
antiviral
effects
through
binding
N
protein
SARS-CoV-2.
This
review
provides
an
account
of
the
tryptophan-specific
conjugation
peptides
and
proteins
its
extensive
application
in
imaging
living
cells,
radiolabelling
proteins,
protein
engineering,
etc
.
Journal of the American Chemical Society,
Journal Year:
2021,
Volume and Issue:
144(1), P. 23 - 41
Published: Dec. 30, 2021
Although
electrochemical
strategies
for
small-molecule
synthesis
are
flourishing,
this
technology
has
yet
to
be
fully
exploited
the
mild
and
chemoselective
modification
of
peptides
proteins.
With
growing
number
diverse
peptide
natural
products
being
identified
emergence
modified
proteins
as
therapeutic
diagnostic
agents,
methods
stand
alluring
prospects
harnessing
reactivity
polypeptides
build
molecular
complexity.
As
a
inherently
tunable
reaction
platform,
electrochemistry
is
arguably
well-suited
overcome
chemo-
regioselectivity
issues
which
limit
existing
bioconjugation
strategies.
This
Perspective
will
showcase
recently
developed
approaches
protein
modification.
The
article
also
highlights
wealth
untapped
opportunities
production
homogeneously
biomolecules,
with
an
eye
toward
realizing
enormous
potential
chemistry.
Chemical Science,
Journal Year:
2022,
Volume and Issue:
13(9), P. 2551 - 2573
Published: Jan. 1, 2022
Pd-catalysed
C–H
functionalisation
of
free
carboxylic
acids
has
drawn
significant
attention
over
the
last
few
years
due
to
predominance
acid
moieties
in
pharmaceuticals
and
agrochemicals.
Acta Pharmaceutica Sinica B,
Journal Year:
2023,
Volume and Issue:
14(3), P. 1030 - 1076
Published: Nov. 18, 2023
Synthetic
chemistry
plays
an
indispensable
role
in
drug
discovery,
contributing
to
hit
compounds
identification,
lead
optimization,
candidate
drugs
preparation,
and
so
on.
As
Nobel
Prize
laureate
James
Black
emphasized,
"the
most
fruitful
basis
for
the
discovery
of
a
new
is
start
with
old
drug"
Chemical Communications,
Journal Year:
2023,
Volume and Issue:
59(23), P. 3383 - 3398
Published: Jan. 1, 2023
This
review
aims
to
provide
an
overview
of
recent
advances
in
the
field
functional
peptide-based
biosensing
cancer
biomarkers.
Particular
attention
is
focused
on
use
electrochemical
and
optical
techniques.
Angewandte Chemie International Edition,
Journal Year:
2021,
Volume and Issue:
61(7)
Published: Oct. 21, 2021
Hypervalent
iodine
compounds
are
powerful
reagents
for
the
development
of
novel
transformations.
As
they
exhibit
low
toxicity,
high
functional
group
tolerance,
and
stability
in
biocompatible
media,
have
been
used
functionalization
biomolecules.
Herein,
we
report
recent
advances
up
to
June
2021
peptide
protein
modification
using
hypervalent
reagents.
Their
use
as
transfer
or
oxidizing
is
discussed
this
Minireview,
including
methods
targeting
polar,
aromatic,
aliphatic
amino
acids
termini.
Chemical Science,
Journal Year:
2022,
Volume and Issue:
13(10), P. 2809 - 2823
Published: Jan. 1, 2022
This
perspective
highlights
the
growing
body
of
literature
that
leverages
polarity
reversal
(umpolung
reactivity)
for
selective
modification
proteinogenic
functionalities
and
identifies
opportunities
further
innovation.
ACS Central Science,
Journal Year:
2023,
Volume and Issue:
9(4), P. 756 - 762
Published: March 27, 2023
Direct
functionalization
of
inert
C-H
bonds
is
one
the
most
attractive
yet
challenging
strategies
for
constructing
molecules
in
organic
chemistry.
Herein,
we
disclose
an
unprecedented
and
Earth
abundant
Cu/Cr
catalytic
system
which
unreactive
alkyl
are
transformed
into
nucleophilic
alkyl-Cr(III)
species
at
room
temperature,
enabling
carbonyl
addition
reactions
with
strong
bonds.
Various
aryl
alcohols
furnished
under
mild
reaction
conditions
even
on
a
gram
scale.
Moreover,
this
new
radical-to-polar
crossover
approach
further
applied
to
1,1-difunctionalization
aldehydes
alkanes
different
nucleophiles.
Mechanistic
investigations
reveal
that
aldehyde
not
only
acts
as
reactant
but
also
serves
photosensitizer
recycle
Cu
Cr
catalysts.
Advanced Synthesis & Catalysis,
Journal Year:
2022,
Volume and Issue:
364(8), P. 1371 - 1387
Published: March 11, 2022
Abstract
2‐Bromo‐3,3,3‐trifluoropropene
(BTP)
represents
a
highly
valuable
synthon
in
synthetic
chemistry,
and
has
been
widely
used
organic
synthesis,
mainly
including
addition
reactions,
cross‐coupling
cycloaddition
or
cyclization
S
N
2’
Stetter
reactions
for
the
construction
of
various
fluorinated
compounds.
In
this
review,
we
systematically
summarize
these
reactions;
their
mechanisms
are
also
discussed.
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