Direct gem‐Difluoroalkenylation of X−H Bonds with Trifluoromethyl Ketone N‐Triftosylhydrazones for Synthesis of Tetrasubstituted Heteroatomic gem …

X Zhang, L Li, G Zanoni, X Han… - Chemistry–A European …, 2022 - Wiley Online Library
The direct gem‐difluoroalkenylation of X− H bonds represents the most straightforward
approach to access heteroatomic gem‐difluoroalkenes that, as the isostere of the carbonyl …

Highly electrophilic silver carbenes

X Zhang, L Li, P Sivaguru, G Zanoni, X Bi - Chemical Communications, 2022 - pubs.rsc.org
Catalytic carbene transfer reactions are fundamental transformations in modern organic
synthesis, which enable direct access to diverse structurally complex molecules. Despite …

Synthesis of Unsymmetrical Squaramides as Allosteric GSK‐3β Inhibitors Promoting β‐Catenin‐Mediated Transcription of TCF/LEF in Retinal Pigment Epithelial Cells

G Carullo, L Bottoni, S Pasquini, A Papa… - …, 2022 - Wiley Online Library
The glycogen synthase kinase 3β (GSK‐3β) is a ubiquitous enzyme that is a validated target
for the development of potential therapeutics useful in several diseases including retinal …

Synthesis and Investigation of Backbone Modified Squaramide Dipeptide Self-Assembly

SD Shinde, N Kulkarni, B Sahu - ACS Applied Bio Materials, 2023 - ACS Publications
Dipeptides are minimalistic peptide building blocks that form well ordered structures through
molecular self-assembly. The driving forces involved are cooperative noncovalent …

[HTML][HTML] Thermodynamic Overview of Bioconjugation Reactions Pertinent to Lysine and Cysteine Peptide and Protein Residues

M Lopandic, F Merza, JF Honek - Compounds, 2023 - mdpi.com
Bioconjugation reactions are critical to the modification of peptides and proteins, permitting
the introduction of biophysical probes onto proteins as well as drugs for use in antibody …

Squaramide Formation for DNA-Encoded Library Synthesis

A Douchez, J Poupart, G Yang… - Bioconjugate …, 2024 - ACS Publications
DNA-encoded libraries (DELs) can be considered as one of the most powerful tools for the
discovery of small molecules of biological interest. However, the ability to access large DELs …

Bifunctional backbone modified squaramide dipeptides as amyloid beta (Aβ) aggregation inhibitors

SD Shinde, SK Behera, N Kulkarni, B Dewangan… - Bioorganic & Medicinal …, 2024 - Elsevier
Alzheimer's disease (AD) is a devastating neurodegenerative condition with complex
pathophysiology. Aggregated amyloid beta (Aβ) peptide plaques and higher concentrations …

σ‐Electrons Responsible for Cooperativity and Ring Equalization in Hydrogen‐Bonded Supramolecular Polymers

L de Azevedo Santos, D Cesario, P Vermeeren… - …, 2022 - Wiley Online Library
We have quantum chemically analyzed the cooperative effects and structural deformations
of hydrogen‐bonded urea, deltamide, and squaramide linear chains using dispersion …

Introducing a squaramide-based self-immolative spacer for controlled drug release

M Ximenis, A Sampedro, L Martínez-Crespo… - Chemical …, 2021 - pubs.rsc.org
Herein we report the design, synthesis and assessment of the first example of a squaramide-
based self-immolative system triggered by an enzymatic reduction. We have proved that the …

Squaryl group-modified UDP analogs as inhibitors of the endoplasmic reticulum-resident folding sensor enzyme UGGT

J Abe, Y Takeda, T Kikuma, Y Kizuka… - Chemical …, 2023 - pubs.rsc.org
UDP-Glc: glycoprotein glucosyltransferase (UGGT) has a central role to retain quality control
of correctly folded N-glycoprotein in the endoplasmic reticulum (ER). A selective and potent …