Results 21 to 30 of about 6,559 (227)
Molecules, 2022 Macrocycles represent attractive candidates in organic synthesis and drug discovery. Since 2014, nineteen macrocyclic drugs, including three radiopharmaceuticals, have been approved by FDA for the treatment of bacterial and viral infections, cancer ...
Dianqing Sun
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Structural basis of ribosomal peptide macrocyclization in plants
eLife, 2018 Constrained, cyclic peptides encoded by plant genes represent a new generation of drug leads. Evolution has repeatedly recruited the Cys-protease asparaginyl endopeptidase (AEP) to perform their head-to-tail ligation. These macrocyclization reactions use
Joel Haywood +7 more
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Pharmaceuticals, 2023 Kinases play an important role in regulating various intracellular signaling pathways that control cell proliferation, differentiation, survival, and other cellular processes, and their deregulation causes more than 400 diseases.
Swapnil P. Bhujbal, Jung-Mi Hah
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Macrocyclization of native peptides through (thio)urea crosslinking of two amines. [PDF]
Nat CommunCyclopeptides have emerged as promising candidates for drug development. However, owing to the scarcity of efficient cyclization strategies for natural peptides, the development of diverse cyclopeptides remains a formidable challenge.
Liu J +10 more
europepmc +2 more sources
Hybrid Macrocyclic Peptides - Synthetic Strategies to Diversify and Cyclize Peptide Libraries in Phage Display Selections. [PDF]
ChemistryHybrid macrocyclic peptides unite genetically encoded peptide libraries with the structural complexity of synthetic small molecules. This Review critically analyzes phage‐compatible cyclization and diversification chemistries, highlights emerging opportunities beyond traditional cysteine‐based approaches, and outlines how future advances may enable the
Oppewal TR, Mayer C.
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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
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, 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. +10 more
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Atroposelective Synthesis of Isoriccardin C through a C−H Activated Heck Type Macrocyclization [PDF]
, 2021 Macrocyclization is typically the key step in syntheses of cyclophane‐type natural products. Considering compounds with axially chiral biaryl moieties, the control of atroposelectivity is essential for biological activity and is synthetically challenging.
Choppin, Sabine +4 more
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Applied Sciences, 2022 The study’s aim was to synthesize new unsymmetrical sulfanyl zinc(II) porphyrazines and subject them to physicochemical and electrochemical characterization and also an initial acute toxicity assessment.
Patrycja Koza +3 more
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Beilstein Journal of Organic Chemistry, 2010 Two procedures for the synthesis of benzo-21-crown-7 have been explored. The [1+1] macrocyclization with KBF4 as the template was found to be more efficient than the intramolecular macrocyclization without template.
Wei Jiang, Christoph A. Schalley
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