[PDF] Progress Towards The Total Synthesis Of Nogalamycin And Expanding The Scope Of Heterocycles In Dna Encoded Libraries eBook

Author : Hillary Dequina
Publisher :
Page : 0 pages
File Size : 20,62 MB
Release : 2023
Category :
ISBN :

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Nogalamycin is an anthracycline natural product that has displayed potent inhibitionagainst gram positive bacteria and prominent toxicity against cancer cell lines. Nogalamycin differs from other anthracyclines with the addition of a unique bicyclic aminosugar tethered to its D-ring. Herein, we will describe a highly modular and convergent route towards the first total synthesis of Nogalamycin. Though reports of toxicity in mammals halted further clinical studies of Nogalamycin, we envision modifying our synthesis toward the preparation of nogalamycin analogs to further demonstrate the high modularity and versatility afforded by our approach. Chapter 1 serves as an introduction by providing a selected review of synthetic strategies toward Nogalamycin, Menogaril, and partial syntheses of their key fragments. Chapter 2 discusses the initial progress toward the total synthesis of Nogalamycin. Alternate strategies to ring-open a difficult oxabicyclic alkene are explored. Arguably the bottleneck of the design-make-test platform for drug discovery and development is its fundamental goal: the identification and validation of specific ligands against pharmaceutically relevant targets. Improved methods for rapid and efficient identification of binders of traditionally challenging targets are highly sought after. As DNA encoded libraries (DELs) are establishing themselves as a promising drug discovery platform, new DNA-compatible reactions are highly sought after to increase the diversity in library development and increase the potential hits against targets of interest. Chapter 3 presents a short overview on DELs including a discussion on their construction as well as their advances made and current limitations. Chapter 4 introduces investigations of aziridinium ylide reactivity and focuses on attempts to incorporate the aziridinium ylide-derived dehydropiperidines as a unique building block scaffold for DELs. Chapter 5 explores the development of a novel oxidative, threecomponent coupling on-DNA.

Author : Christopher T. Walsh
Publisher : Royal Society of Chemistry
Page : 787 pages
File Size : 47,38 MB
Release : 2017-04-28
Category : Science
ISBN : 1788010760

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This textbook describes the types of natural products, the biosynthetic pathways that enable the production of these molecules, and an update on the discovery of novel products in the post-genomic era.

Author : Lixin Zhang
Publisher : Springer Science & Business Media
Page : 380 pages
File Size : 19,89 MB
Release : 2007-11-17
Category : Medical
ISBN : 1592599761

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A fresh examination of the past successes of natural products as medicines and their new future from both conventional and new technologies. High-performance liquid chromatography profiling, combinatorial synthesis, genomics, proteomics, DNA shuffling, bioinformatics, and genetic manipulation all now make it possible to rapidly evaluate the activities of extracts as well as purified components derived from microbes, plants, and marine organisms. The authors apply these methods to new natural product drug discoveries, to microbial diversity, to specific groups of products (Chinese herbal drugs, antitumor drugs from microbes and plants, terpenoids, and arsenic compounds), and to specific sources (the sea, rainforest, and endophytes). These new opportunities show how research and development trends in the pharmaceutical industry can advance to include both synthetic compounds and natural products, and how this paradigm shift can be more productive and efficacious.

Author : Gordon M. Cragg
Publisher : CRC Press
Page : 610 pages
File Size : 27,75 MB
Release : 2005-06-13
Category : Medical
ISBN : 1420039652

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Plants, marine organisms, and microorganisms have evolved complex chemical defense and signaling systems that are designed to protect them from predators and provide other biological benefits. These organisms thus produce substances containing novel chemotypes that may have beneficial effects for humans. As collection methods improve and new screen

Author : L. Dogliotti
Publisher : Springer
Page : 311 pages
File Size : 36,38 MB
Release :
Category : Medical
ISBN : 9781461534952

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The fight against breast cancer is expected to be effectively stimulated by interdisciplinary approaches and cross-fertilization between laboratory and clinical research findings. Of major importance are therefore meetings promoting fast transfer to clinical applications of findings by basic scientists. The present volume, reporting the proceedings of the 1991 Biennial Conference of the International Association for Breast Cancer Research, hopes to achieve this goal by presenting the most recent observations in the laboratory and their possible applications for diagnostic evaluations and clinical treatments. The sections of the book focus first on the oncogenes more likely involved in mammary tumorigenesis and on the polypeptide factors and steroid hormones affecting proliferation and possibly inducing carcinogenesis in breast epithelium. A section is devoted to the epidemiological studies and to the identification of risk factors, a way to select populations at higher risk and, possibly, to help in preventing the disease. Special emphasis is given to the establishment of diagnostic criteria and to the selection of prognostic factors, which must support an effective therapeutic planning. It is our hope that this volume, a timely update of the most recent advances in specific fields presented by basic scientists, pathologists and clinicians will stimulate new insights and progresses leading ultimately to the control of breast cancer.

Author :
Publisher : Academic Press
Page : 644 pages
File Size : 18,17 MB
Release : 2009-04-11
Category : Science
ISBN : 0080923364

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Microbial natural products have been an important traditional source of valuable antibiotics and other drugs but interest in them waned in the 1990s when big pharma decided that their discovery was no longer cost-effective and concentrated instead on synthetic chemistry as a source of novel compounds, often with disappointing results. Moreover understanding the biosynthesis of complex natural products was frustratingly difficult. With the development of molecular genetic methods to isolate and manipulate the complex microbial enzymes that make natural products, unexpected chemistry has been revealed and interest in the compounds has again flowered. This two-volume treatment of the subject will showcase the most important chemical classes of complex natural products: the peptides, made by the assembly of short chains of amino acid subunits, and the polyketides, assembled from the joining of small carboxylic acids such as acetate and malonate. In both classes, variation in sub-unit structure, number and chemical modification leads to an almost infinite variety of final structures, accounting for the huge importance of the compounds in nature and medicine. Gathers tried and tested methods and techniques from top players in the field Provides an extremely useful reference for the experienced research scientist Covers biosynthesis of Polyketides, Tarpenoids, Aminocoumarins and Crabohydrates

Author : Paul J. Scheuer
Publisher : Springer
Page : 212 pages
File Size : 10,72 MB
Release : 1993-07-23
Category : Science
ISBN :

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1. B.J. Baker, R.G. Kerr: Biosynthesis of Marine Sterols 2. C.W.J. Chang, P.J. Scheuer: Marine Isocyano Compounds 3. G. Cimino, G. Sodano: Biosynthesis of Secondary Metabolites in Marine Molluscs 4. W.H. Gerwick, D.G. Nagle, P.J. Proteau: Oxylipins from Marine Invertebrates

Author : Sekhar Chandra Ray
Publisher : Elsevier
Page : 252 pages
File Size : 15,77 MB
Release : 2017-03-07
Category : Technology & Engineering
ISBN : 0323479073

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Nanomaterials for Biological and Medical Applications explores the different applications of carbon nanomaterials in drug and gene therapies and their use in tissue regeneration, biosensor diagnosis, enantiomer separation of chiral drugs, extraction and analysis of drugs and pollutants, and as antitoxents. The book describes the synthesis processing of carbon nanomaterials, carbon composite nanomaterials, and their different biological and biomedical applications, including the removal of biologically toxic materials, optical biosensor applications, bio-imaging probe, drug delivery, cancer treatments, and other biomedical applications. Explains the major synthesis chemical process of carbon nanomaterials for biological applications Discusses how carbon nanomaterials can be practically used to create more efficient nanodevices in biosensing, medical imaging, and drug delivery Explores how the unique physical properties of carbon nanomaterials allows them to remove biologically toxic materials

Author : S. Grabley
Publisher : Springer Science & Business Media
Page : 380 pages
File Size : 24,10 MB
Release : 1998-11-26
Category : Medical
ISBN : 9783540648444

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This book is unique in covering the present status and future potential of natural products in drug discovery. It provides readers with recent information regarding the impact on drug discovery, development and strategies, technical and automation aspects, and methods based on biochemistry as well as molecular biology, highlighting compounds from natural sources. Special emphasis is placed on the various strategies to gain access to natural compounds and combinatorial approaches by making use of both synthetic and biological methods.