Results 11 to 20 of about 442 (127)
Total Syntheses of Colletopeptide A and Colletotrichamide A
The first total syntheses of cyclic depsipeptides colletopeptide A and colletotrichamide A, have been accomplished. The key advanced intermediate, a cyclic tridepsipeptide derivative, was constructed using a sequence of transformations that features ...
Jing Chen +4 more
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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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Synthesis of a versatile metacyclophane macrolactam [PDF]
As Hsp90 has emerged as a promising target for the development of cancer chemotherapeutics, so has the need for systematic evaluation of structure-activity relationships between natural product inhibitors and this molecular chaperone. Utilizing our chimera approach, which encompasses the quinone moiety of geldanamycin and the resorcinol moiety of ...
Mingwen, Wang, Brian S J, Blagg
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Indole-Based Macrocyclization by Metal-Catalyzed Approaches
This review is dedicated to the different varieties of macrocycles synthesis bearing indole units in their architecture by metal-catalyzed strategies.
Subba Rao Cheekatla +4 more
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Enzymatic Timing and Tailoring of Macrolactamization in Syringolin Biosynthesis [PDF]
The enzymatic activation of 3,4-dehydrolysine and subsequent formation of the 12-membered syringolin macrolactam were investigated. The timing of the desaturation was elucidated through the analysis of the initial adenylation domain of SylD. The SylD-TTE didomain was characterized and demonstrated to be the catalyst for formation of 12-membered ...
Wuest, William M. +3 more
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Polycyclic Tetramate Macrolactams—A Group of Natural Bioactive Metallophores [PDF]
New infectious diseases and increase in drug-resistant microbial pathogens emphasize the need for antibiotics with novel mode-of-action. Tetramates represented by fungi-derived tenuazonic acid and bacterial polycyclic tetramate macrolactams (PTMs) are an important family of natural products with a broad spectrum of antimicrobial activities.
Ding, Ling; id_orcid 0000-0001-8979-3104 +6 more
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Anthelmintic Macrolactams from Nonomuraea turkmeniaca MA7381 [PDF]
A new macrolactam, fluvirucin B0 (1), and two known macrolactams, Sch 38516/fluvirucin B1 (2) and Sch 39185/fluvirucin B3 (3), have been isolated from an acetone extract of a strain of Nonomuraea turkmeniaca. These compounds were isolated by bioassay-guided fractionation as part of our search for new anthelmintics.
Sloan, Ayers +8 more
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Giant Macrolactams Based on β-Sheet Peptides [PDF]
This paper reports the use of natural amino acids, the tripeptide β-strand mimic Hao, and the β-turn mimic δ-linked ornithine to generate water-soluble 54-, 78-, and 102-membered-ring macrolactams. These giant macrocycles were efficiently prepared by synthesis of the corresponding protected linear peptides, followed by solution-phase cyclization and ...
Pin-Nan, Cheng, James S, Nowick
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Macrocyclic Drugs and Synthetic Methodologies toward Macrocycles
Macrocyclic scaffolds are commonly found in bioactive natural products and pharmaceutical molecules. So far, a large number of macrocyclic natural products have been isolated and synthesized.
Xufen Yu, Dianqing Sun
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Recent Reports of Solid-Phase Cyclohexapeptide Synthesis and Applications
Macrocyclic peptides are privileged scaffolds for drug development and constitute a significant portion of macrocyclic drugs on the market today in fields spanning from infectious disease to oncology.
Allan M. Prior +3 more
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