☆ 4.6 Article

Large-scale synthesis of Notum inhibitor 1-(2,4-dichloro-3-(trifluoromethyl)-phenyl)-1H-1,2,3-triazole (ARUK3001185) employing a modified Sakai reaction as the key step

RSC ADVANCES (2022)

Related references

Note: Only part of the references are listed.

Article Chemistry, Multidisciplinary

[4+1] Annulation of in situ generated azoalkenes with amines: A powerful approach to access 1-substituted 1,2,3-triazoles

Hongwei Wang et al.

Summary: This article reports a substrate-based method for the [4 + 1] annulation reaction of azoalkenes generated from readily available difluoroacetaldehyde N-tosylhydrazones (DFHZ-Ts) with amines, leading to the high-yield synthesis of diverse 1-substituted 1,2,3-triazole derivatives under relatively mild conditions.

CHINESE CHEMICAL LETTERS (2022)

Add to Collection

Article Chemistry, Medicinal

Design of a Potent, Selective, and Brain-Penetrant Inhibitor of Wnt-Deactivating Enzyme Notum by Optimization of a Crystallographic Fragment Hit

Nicky J. Willis et al.

Summary: Notum functions as a crucial enzyme in human diseases such as colorectal cancer and Alzheimer's disease. The discovery of 8l as a potent, selective, and brain-penetrant inhibitor of Notum activity suitable for oral dosing in rodent models of disease marks a significant progress in developing improved inhibitors for neurodegenerative diseases.

JOURNAL OF MEDICINAL CHEMISTRY (2022)

Add to Collection

Review Chemistry, Organic

Recent Developments in N 2 -Selective Functionalizations of 1,2,3-Triazoles

Yue Zheng et al.

SYNTHESIS-STUTTGART (2022)

Add to Collection

Review Biochemistry & Molecular Biology

Triazoles and Their Derivatives: Chemistry, Synthesis, and Therapeutic Applications

Mohammed M. Matin et al.

Summary: Triazoles have superior pharmacological applications, accommodating a broad range of substituents for the construction of diverse novel bioactive molecules. They exhibit significant biological properties including antimicrobial, antiviral, anticancer activities. However, careful evaluation of potential side effects is needed for higher efficacy in therapeutic applications.

FRONTIERS IN MOLECULAR BIOSCIENCES (2022)

Add to Collection

Review Chemistry, Multidisciplinary

A Hitchhiker's Guide to Click-Chemistry with Nucleic Acids

Nicolo Zuin Fantoni et al.

Summary: Click chemistry, particularly azide-alkyne cycloadditions, is a powerful technique for the covalent conjugation of molecular entities. Its application in nucleic acid chemistry allows efficient and cost-effective labeling, ligation, and cyclization of oligonucleotides compared to traditional techniques. This review provides a guide to researchers approaching the field, discussing the chemistry and applications of AAC reactions in nucleic acids.

CHEMICAL REVIEWS (2021)

Add to Collection

Article Chemistry, Multidisciplinary

Bioactive 1,2,3-Triazoles: An Account on their Synthesis, Structural Diversity and Biological Applications

Luana da S. M. Forezi et al.

Summary: The triazole heterocycle is a privileged scaffold in medicinal chemistry, and various methods for its preparation are described. This paper discusses the development of new methods for the synthesis of 1,2,3-triazoles and the preparation of new triazole-functionalized biologically active molecules using classical approaches, highlighting the significant contributions from the research group in this field.

CHEMICAL RECORD (2021)

Add to Collection

Article Chemistry, Medicinal

Carboxylesterase Notum Is a Druggable Target to Modulate Wnt Signaling

Elliott D. Bayle et al.

Summary: Regulation of the Wnt signaling pathway is crucial for various cellular processes in both development and adult mammalian biology. Inhibiting Notum activity may provide a new approach for treating diseases where aberrant Notum activity is the underlying cause. Reliable screening technologies and structural studies are accelerating the discovery of new Notum inhibitors.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

Add to Collection

Article Chemistry, Medicinal

Small-molecule inhibitors of carboxylesterase Notum

Yuguang Zhao et al.

Summary: Notum has been identified as a negative regulator of Wnt signaling by removing an essential palmitoleate group from Wnt proteins. It plays a role in human diseases, and targeting Notum with small-molecule inhibitors has shown promising results in treating cancer, osteoporosis, and neurodegenerative disorders. Various successful hit-finding strategies, including high-throughput screening and structural studies, have been applied to accelerate the discovery of new inhibitors of Notum.

FUTURE MEDICINAL CHEMISTRY (2021)

Add to Collection

Article Multidisciplinary Sciences

NOTUM from Apc-mutant cells biases clonal competition to initiate cancer

Dustin J. Flanagan et al.

Summary: The tumour suppressor APC is the most commonly mutated gene in colorectal cancer. Loss of Apc in intestinal stem cells drives the formation of adenomas in mice via increased WNT signalling, while reduced secretion of WNT ligands increases the ability of Apc-mutant intestinal stem cells to colonize a crypt. The study found that Apc-mutant cells are enriched for transcripts encoding several secreted WNT antagonists, with Notum being the most highly expressed. These cells actively inhibit the proliferation of surrounding wild-type crypt cells, outcompeting them in the niche and driving their differentiation.

NATURE (2021)

Add to Collection

Article Chemistry, Multidisciplinary

A Scalable Metal-, Azide-, and Halogen-Free Method for the Preparation of Triazoles

Peter R. Clark et al.

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2020)

Add to Collection

Article Chemistry, Organic

An azide and acetylene free synthesis of 1-substituted 1,2,3-triazoles

Sarah J. M. Patterson et al.

TETRAHEDRON LETTERS (2020)

Add to Collection

Article Cell & Tissue Engineering

NOTUM inhibition increases endocortical bone formation and bone strength

Robert Brommage et al.

BONE RESEARCH (2019)

Add to Collection

Article Chemistry, Medicinal

Selective Irreversible Inhibitors of the Wnt-Deacylating Enzyme NOTUM Developed by Activity-Based Protein Profiling

Radu M. Suciu et al.

ACS MEDICINAL CHEMISTRY LETTERS (2018)

Add to Collection

Review Biochemistry & Molecular Biology

Wnt/β-Catenin Signaling, Disease, and Emerging Therapeutic Modalities

Roel Nusse et al.

CELL (2017)

Add to Collection

Article Chemistry, Medicinal

Stimulation of cortical bone formation with thienopyrimidine based inhibitors of Notum Pectinacetylesterase

James E. Tarver et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2016)

Add to Collection

Article Cell Biology

Notum Is Required for Neural and Head Induction via Wnt Deacylation, Oxidation, and Inactivation

Xinjun Zhang et al.

DEVELOPMENTAL CELL (2015)

Add to Collection

Article Multidisciplinary Sciences

Notum deacylates Wnt proteins to suppress signalling activity

Satoshi Kakugawa et al.

NATURE (2015)

Add to Collection

Article Chemistry, Multidisciplinary

Traceless Tosylhydrazone-Based Triazole Formation: A Metal-Free Alternative to Strain-Promoted Azide-Alkyne Cycloaddition

Sander S. van Berkel et al.

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2012)

Add to Collection

Article Chemistry, Multidisciplinary

Highly N-2-Selective Palladium-Catalyzed Arylation of 1,2,3-Triazoles

Satoshi Ueda et al.

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2011)

Add to Collection

Article Chemistry, Organic

Solvent-free copper/iron co-catalyzed N-arylation reactions of nitrogen-containing heterocycles with trimethoxysilanes in air

Ren-Jie Song et al.

TETRAHEDRON LETTERS (2007)

Add to Collection

© Peeref 2019-2024. All rights reserved.