Studies Towards the Total Synthesis of the Epothilones A and B. PDF Download
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Author: Jane Elaine Fletcher
Publisher:
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Category :
Languages : en
Pages :
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Author: Jane Elaine Fletcher
Publisher:
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Category :
Languages : en
Pages :
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Author: Raphael Schiess
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Category :
Languages : en
Pages :
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Author:
Publisher:
ISBN:
Category :
Languages : en
Pages : 108
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Epothilones are a class of promising anti breast cancer candidate. They were synthesized by four strategies. Structure - activity relationships were studied with the synthetic compounds. The first in vivo test of synthetic epothilone D is encouraging.
Author: Benjamin Anthony Pratt
Publisher: ProQuest
ISBN: 9780549876021
Category : Diterpenes
Languages : en
Pages : 384
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As the first epothilone analogue has recently been approved for clinical use by the FDA, the epothilones stand on the verge of becoming the standard for chemotherapeutic care. A new batch of designed Epothilone B analogues has been synthesized that possess broad structural diversity on the heterocyclic sidechain and unrivaled biological activity against drug-susceptible and drug-resistant cell lines. The most potent epothilone analogues from this study are currently under development toward becoming clinical candidates. Progress has been made toward the total synthesis of the complex and biologically active norcembranoid class of Sinularia natural products. Development of a convergent synthesis to a common, key intermediate has allowed for the near completion of Norcembranolide and Sinuleptolide. Within this synthetic strategy is the development of a novel rhodium-catalyzed macrocyclic ring closing reaction and a palladium-mediated acetylenic ketone rearrangement to 2,5-furans. This synthetic strategy provides access to the key intermediate of 8 complex natural products in the norcembrane, yonarane and dimeric-norcembrane families.
Author: Goutam Brahmachari
Publisher: Elsevier
ISBN: 0128212780
Category : Science
Languages : en
Pages : 386
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Discovery and Development of Anti-Breast Cancer Agents from Natural Products presents cutting-edge research advances in the field of bioactive natural products and natural drug formulations. This volume in the Natural Products Drug Discovery series focuses on molecules of natural origin and their synthetic analogs that show promising potential to act as anti-breast cancer and chemotherapeutic agents. Combining foundational background information on cancer mechanisms with details of medicinal structures from natural products, this volume compiles the latest developments from across interdisciplinary fields.Discovery and Development of Anti-Breast Cancer Agents from Natural Products will serve as a valuable resource for researchers working to discover promising leads for the development of novel pharmaceuticals for breast cancer, highlighting a number of key structures from natural products and exploring possible future developments in the area. - Highlights active agents from natural sources for development as novel anti-cancer agents - Features contributions from active researchers and leading experts working in the field - Includes foundational background information on both breast cancer mechanisms and natural product structures to support researchers from different disciplines
Author: Nathaniel George Martin
Publisher:
ISBN:
Category :
Languages : en
Pages : 213
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Author: Johann H. Mulzer
Publisher: Springer Science & Business Media
ISBN: 3211782079
Category : Science
Languages : en
Pages : 266
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Epothilones have received unusual attention over the past ten years. They are novel antitumor drugs which very much like their predecessor paclitaxel (Taxol) act via microtubule stabilization. In comparison to paclitaxel and a number of alternative drugs with a similar mode of bioaction (e.g. laulimalide, eleutherobin, peluroside, discodermolide) the epothilones have significant advantages, above all very high activity in the nanomolar range and low susceptibility towards multidrug resistance. Epothilone B and several derivatives thereof are in phase I-III clinical trials; one of them (ixabepilone, BMS) is already on the market, others are supposed to appear on the market in the near future. All naturally occurring epothilones have been isolated from Sorangium cellulosum; their antitumor action is traced back to the stabilization of microtubules. In consequence, the formation of the mitototic spindle is prohibited and the cell undergoes apoptosis.
Author: Jiri Kasparec
Publisher:
ISBN:
Category :
Languages : en
Pages : 148
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Author: Eric L. Williams
Publisher:
ISBN:
Category : Organic compounds
Languages : en
Pages : 164
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Author: Naim Nazef
Publisher:
ISBN:
Category :
Languages : en
Pages :
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Merrilactone A (1) and the epimeric anislactones A (2) and B (3) are sesquiterpene natural products that were first isolated from the dried pericarps of Illicium merrillianum (Fukuyama in 2000) and Illicium anisatum (Kouno in 1990), respectively. Merrilactone A (1) was identified as a potent nonpeptidal neurotrophic factor that strongly promotes neurite outgrowth in the culture of foetal rat cortical neurons and is a potential small molecule lead for the treatment of neurodegenerative disorders. Merrilactone A (1) together with 2 and 3, are highly complex cage-like structures that have established themselves as challenging and attractive targets in natural product synthesis. Presented in this research is a regiodivergent approach to both sets of natural products via the first known application of the defining transformation, an intramolecular tandem cyano-aldol cyclisation. We demonstrated an efficient route to the cyano-aldol product 303, which acted as the common intermediate to either natural product by orthogonal lactonisation sequences. This culminated in the successful synthesis of known intermediate 320, which represents the formal total synthesis of 1, and advanced tetracyclic intermediate 309, that is the full carbon skeleton of 2 and 3.
