BIOACTIVE NATURAL PRODUCTS Opportunities and Challenges in Medicinal Chemistry 8033hc.9789814335379-tp.indd 1 8/29/11 10:32 AM BIOACTI V E NATURAL PRODUCTS Opportunities and Challenges in Medicinal Chemistry editor Goutam Brahmachari Visva-Bharati University, India World Scientific NEW JERSEY • LONDON • SINGAPORE • BEIJING • SHANGHAI • HONG KONG • TAIPEI • CHENNAI 8033hc.9789814335379-tp.indd 2 8/29/11 10:32 AM Published by World Scientific Publishing Co. Pte. Ltd. 5 Toh Tuck Link, Singapore 596224 USA office: 27 Warren Street, Suite 401-402, Hackensack, NJ 07601 UK office: 57 Shelton Street, Covent Garden, London WC2H 9HE British Library Cataloguing-in-Publication Data A catalogue record for this book is available from the British Library. BIOACTIVE NATURAL PRODUCTS Opportunities and Challenges in Medicinal Chemistry Copyright © 2012 by World Scientific Publishing Co. Pte. Ltd. All rights reserved. This book, or parts thereof, may not be reproduced in any form or by any means, electronic or mechanical, including photocopying, recording or any information storage and retrieval system now known or to be invented, without written permission from the Publisher. For photocopying of material in this volume, please pay a copying fee through the Copyright Clearance Center, Inc., 222 Rosewood Drive, Danvers, MA 01923, USA. In this case permission to photocopy is not required from the publisher. ISBN-13 978-981-4335-37-9 ISBN-10 981-4335-37-1 Typeset by Stallion Press Email: [email protected] Printed in Singapore. Jihan - Bioactive Natural Products.pmd 1 10/14/2011, 9:09 AM b1214_FM.qxd 8/24/2011 5:41 PM Page v b1214 Bioactive Natural Products To All those who are working globally with bioactive natural products for the cause of human welfare b1214_FM.qxd 8/24/2011 5:41 PM Page vii b1214 Bioactive Natural Products Foreword Unlike other books with a similar title, this edited volume covers not only secondary metabolites from natural product sources and their derivatives, but also a significant amount of what might best be covered under the rubric of alternative medicine or even functional food stuffs. In addition, it also contains excellent chapters on the methodologies of production of “natural products that will be drug molecules in their own right”. Thus there are chapters by well-known experts on not only classical fermenta- tion processes using microbes, but also on the methodologies involved in plant tissue culture. This latter system is one that is not often referred to for drug production, but over the last 5+ years, it has become a major method for the production of the antitumor drug Taxol® by BristolMyers Squibb. Apoint that is often forgotten in westernized medicine is that of the approximate 7 billion people in the world at this moment, more than 80% of them do not have routine access to drugs as they are defined in Western medicine, but rely upon predominately plant-based therapies as their sources of medicinal agents. Even in areas of the world where single agent drugs are available, traditional therapeutic regimens such as Ayurveda in India, Traditional Chinese Medicine, and Japanese and Korean herbals are still the major source of medicinals. Thus in this volume, as a result of a careful juxtaposition of what might be called “classical natural product-based drug discovery” where pure single compounds or their close chemical relatives, are used as eth- ical pharmaceutical agents, with commentaries on the history and use of agents found in “functional foods and alternative therapies”, the reader will have a more nuanced understanding of the role that natural vii b1214_FM.qxd 8/24/2011 5:41 PM Page viii b1214 Bioactive Natural Products viii Foreword products, in the widest sense of the term, has had upon the discovery and development of agents — be they single agents, or validated mixtures, that can be utilized to maintain the health of people from all areas of the world. David J. Newman Wayne, Pennsylvania, USA June, 2011 b1214_FM.qxd 8/24/2011 5:41 PM Page ix b1214 Bioactive Natural Products Preface This single volume entitled Bioactive Natural Products: Opportunities & Challenges in Medicinal Chemistryis an endeavor to underline how nat- ural product research continues to make significant contributions in the domain of discovery and development of new medicinal entities; the pres- ent book brings together a total of fourteen articles contributed by eminent natural product chemists from several countries in response to my per- sonal invitation. I am most grateful to the authors for their generous and timely response in spite of their busy and tight schedules with academics, research, and other responsibilities. Nature stands as an inexhaustible source of novel chemotypes and pharmacophores; natural products present in the plant and animal king- dom offer a large diversity of chemical structures which are the result of biosynthetic processes that have been modulated over the millennia through genetic effects. Interest in obtaining biologically active com- pounds from natural sources has recently spiked due to their low toxicity, availability from renewable sources, complete biodegradabil- ity, and in most cases, low cost as well. Bioactive natural products are proving to be a rich source of novel therapeutics. The search for bioac- tive molecules from nature (plants, animals, microflora) continues to play an important role in fashioning new medicinal agents. With the advent of modern techniques, particularly the rapid improvements in spectroscopic as well as accompanying advances in high-throughput screening techniques, it has become possible to have an enormous repository of bioactive natural compounds, thus opening up exciting new opportunities in the field of new drug development to the pharma- ceutical industry. Medicinal chemistry of bioactive natural products spans a wide range of fields, including isolation and characterization of bioactive compounds from natural sources, structure modification for optimization of their ix
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