Application of a macrocyclization strategy in kinase inhibitor development [PDF]
Acta Materia MedicaKinases have a pivotal role in phosphorylation and kinase dysregulation has been implicated in the occurrence and progression of various diseases. By mid-2024 the Food and Drug Administration had approved 81 small-molecule kinase inhibitors targeting ...
Kun Xing +5 more
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Double click macrocyclization with Sondheimer diyne of aza-dipyrrins for B–Free bioorthogonal imaging [PDF]
, 2023 Sequential azide/diyne cycloadditions proved highly effective for the macrocyclization of a bis-azido aza-dipyrrin. Macrocyclic aza-dipyrrin could be produced in 30 min at rt in water with changes in fluorescence intensity and lifetimes measurable upon ...
O’Shea, Donal F. +5 more
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Genetic Encoding of Cyanopyridylalanine for In-Cell Protein Macrocyclization by the Nitrile-Aminothiol Click Reaction [PDF]
, 2021 Cyanopyridylalanines are non-canonical amino acids that react with aminothiol compounds under physiological conditions in a biocompatible manner without requiring added catalyst.
Colin, Jackson +7 more
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Spontaneous and Selective Macrocyclization in Nitroaldol Reaction Systems [PDF]
, 2023 Through a dynamic polymerization and self-sorting process, a range of lowellane macrocycles have been efficiently generated in nitroaldol systems composed of aromatic dialdehydes and aliphatic or aromatic dinitroalkanes. All identified macrocycles show a
Mubarak, Ayinla +3 more
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Chirality-Matched Catalyst-Controlled Macrocyclization Reactions [PDF]
, 2021 Macrocycles, formally defined as compounds that contain a ring with 12 or more atoms, continueto attract great interest due to their important applications in physical, pharmacological andenvironmental sciences.
Scott, Miller +2 more
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Multicopper Clusters Catalyze the Oxidative Phenol Macrocyclization (OxPM) of Linear Peptides [PDF]
, 2023 The biosynthesis of glycopeptide antibiotics such as vancomycin and other biologically active biaryl-bridged and diaryl ether-linked macrocyclic peptides includes key enzymatic oxidative phenol macrocyclization(s) of linear precursors.
Mor, Ben-Lulu +8 more
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Peptide macrocyclization by transition metal catalysis [PDF]
, 2020 Peptide macrocyclization has traditionally relied on lactam, lactone and disulfide bond-forming reactions that aim at introducing conformational constraints into small peptide sequences.
Ojeda-Carralero G.M. +3 more
core +3 more sources
Polycavernoside A: The Prins Macrocyclization Approach [PDF]
, 2016 Polycavernoside A: The Prins Macrocyclization ...
Eun Lee (418436) +1 more
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Kinetic Analysis for Macrocyclizations Involving Anionic Template at the Transition State
The Scientific World Journal, 2012 Several kinetic models for the macrocyclization of a C2 pseudopeptide with a dihalide through a SN2 reaction have been developed. These models not only focus on the kinetic analysis of the main macrocyclization reaction, but also consider the competitive
Vicente Martí-Centelles +2 more
doaj +1 more source
Química Nova, 2008 This review presents natural, semi-synthetic and synthetic bioactive macrolactams and their structure-activity relationships when available. For macrolactams in clinical use the advantages and disadvantages in relation to other drugs are presented, and ...
Renata Fontes Prado Faraco +3 more
doaj +1 more source