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Johann H. Mulzer 
The Epothilones: An Outstanding Family of Anti-Tumor Agents 
From Soil to the Clinic

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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.
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Table des matières

General Aspects.- Biosynthesis and Heterologous Production of Epothilones.- Total Synthesis of Epothilones A-F.- Semisynthetic Derivatives of Epothilones.- Preclinical Pharmacology and Structure-Activity Studies of Epothilones.- Clinical Studies with Epothilones.
Langue Anglais ● Format PDF ● Pages 260 ● ISBN 9783211782071 ● Taille du fichier 6.3 MB ● Éditeur Johann H. Mulzer ● Maison d’édition Springer Wien ● Lieu Vienna ● Publié 2009 ● Téléchargeable 24 mois ● Devise EUR ● ID 2155242 ● Protection contre la copie DRM sociale

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