Natural Product Chemistry for Drug Discovery

By: Antony D Buss (Editor), Mark S Butler (Editor)

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Hardcover | 21 October 2009

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Hardcover
458 Pages

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23.5 x 15.88 x 3.18

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Natural Product Chemistry for Drug Discovery provides a comprehensive summary of where natural product chemistry is today in drug discovery. The book covers emerging technologies and case studies and is a source of up-to-date information on the topical subject of natural products. Natural products are once again considered important tools in the drug discovery toolbox. The authors are all experts in their respective fields of natural product chemistry. The book will appeal across the board from scientists to professionals, postgraduates and industrial chemists. The case studies selected for inclusion highlight recently marketed drugs and development candidates that have been derived from natural products. These 'real-life' examples show how new technologies, such as advances in screening, isolation, dereplication and prefractionation, have significantly enhanced the discovery process.

Industry Reviews

"This volume serves as a useful reminder that even as the first decade of the 21st century comes to a close, natural products are still a valuable resource for the new therapeutic agents and new drug leads with broad structural diversity.""This is a timely and highly informative text that belongs in institutional libraries where biomedical research is carried out...many natural product researchers, as well as medicinal chemists, synthetic organic chemists, and pharmacologists will find this volume well worthy of purchase for their personal libraries." * Journal of Medicinal Chemistry, 2010, 53 P2329 *

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Non-Fiction Science Chemistry Organic Chemistry Medicine Nursing & Ancillary Services Pharmacy & Dispensing Other Branches of Medicine Pharmacology Engineering & Technology Industrial Chemistry & Manufacturing Technologies Industrial Chemistry

Pharmaceutical Technology Pre-Clinical Medicine & Basic Sciences

Introduction to Natural Products for Drug Discovery
Natural Products as Drugs and Leads to Drugs: The Historical Perspective
Ancient History (>2900 BCE to 1800 CE)	p. 3
The Initial Influence of Chemistry upon Drug Discovery	p. 6
Alkaloids	p. 6
Aspirin	p. 8
Digitalis	p. 9
20th and 21st Century Drugs/Leads from Nature	p. 10
Antibacterial and Antifungal Antibiotics	p. 10
Antiviral Agents	p. 19
Natural Product Based Antitumour Agents	p. 21
Final Comments	p. 23
References	p. 24
Chemical Space and the Difference Between Natural Products and Synthetics
Introduction	p. 28
Sources of Organic Compounds and Drug Leads	p. 29
Natural Products	p. 29
Natural Product Derivatives	p. 29
Synthetic Compounds	p. 30
Synthetic Compound Libraries	p. 30
Combinatorial Libraries	p. 30
Diversity-Oriented Synthetic (DOS) Libraries	p. 31
Fragment Libraries	p. 31
Lipinski's "Rule, of Five" for Orally Active Drugs	p. 32
Assessment of Diversity of Libraries with Respect to Drugs	p. 33
Molecular Weight	p. 34
Distribution of Atom Types: H-bond Donors and Acceptors	p. 35
Lipophilicities (Log P)	p. 37
Chiral Centres	p. 37
Rotatable Bonds, Unsaturations, Rings, Chains and Ring Topology	p. 38
Principal Component Analysis (PCA)	p. 39
Conclusions	p. 40
References	p. 42
Mechanism of Action Studies
Introduction	p. 44
Some Like It Hot: Esperamicin A₁ Neocarzinostatin and Related Enediyne Antibiotics	p. 45
To Catch a Mockingbird: Taxol, Epothilone and the Microtubule	p. 47
Notorious: Jasplakinolide, Alias Jaspamide and Actin	p. 51
Invasion of the Pathway Snatchers: Artemisinin	p. 53
Once Upon a Time in the Immune System: FK-506, Cyclosporin A and Rapamycin	p. 55
Back to the Cytoskeleton: the Phorboxazoles	p. 56
It's a Wonderful Target: VTPase and its Targeting by Apicularen A, Salicylihalamide A and Palmerolide A	p. 59
Double Indemnity: Bistramide A	p. 61
The Matrix: the Pladienolides and Splicing Factor SF3b	p. 62
The Unusual Suspects: (+)-Avrainvillamide	p. 65
Close Encounters of a Third Kind: Ammosamides, Blebbestatin and Myosin	p. 67
The End	p. 69
References	p. 69
Sources of Compounds
The Convention on Biological Diversity and its Impact on Natural Product Research
Introduction	p. 81
Historical Perspective	p. 85
The Convention on Biological Diversity	p. 87
Implementation and Regulatory Outcomes of the CBD	p. 92
Assessment of Impact	p. 95
An Overview and Some Examples	p. 95
An Informal Survey	p. 100
Survey Results	p. 101
Survey Overview	p. 116
The TRIPS Agreement and the CBD	p. 116
Other Aspects and Outcomes	p. 123
The International Cooperative Biodiversity Group Programme	p. 125
Some Recommendations	p. 127
A Web of Interconnectedness	p. 130
A Different World	p. 131
Conclusions	p. 133
Acknowledgements	p. 134
References	p. 135
Plants: Revamping the Oldest Source of Medicines with Modern Science
Introduction	p. 140
Plant Secondary Metabolites vs. Secondary Metabolites of Other Origin	p. 143
Unnatural Sources of Plant Secondary Metabolites	p. 146
Critical Issues in Plant-based Natural Product Drug Discovery	p. 149
Intellectual Property (IP) Issues	p. 149
Pieiotropy and Synergy	p. 151
Extract Libraries vs. Fraction (Peak) Libraries vs. Compound Libraries	p. 153
Removal of Interfering Compounds	p. 155
Selection Strategies for Plant-Based Natural Product Drug Discovery	p. 156
Ethnopharmacology	p. 156
Zoopharmacy and Animal Toxicology	p. 157
Traditional Medicine	p. 158
Dietary Plants and Spices	p. 159
The Pharmaceutical Relevance of Plants	p. 161
Plants as a Source of Lead Structures and Drugs	p. 161
Plants as a Source of Standardised Extracts	p. 163
Conclusions	p. 167
References	p. 168
Macromarines: A Selective Account of the Potential of Marine Sponges, Molluscs, Soft Corals and Tunicates as a Source of Therapeutically Important Molecular Structures
Introduction	p. 174
Macroorganisms: Outstanding Success in Producing Viable Drug Leads	p. 175
Setting that Ara A and Ara C Story Straight	p. 175
The Potential Role of Invertebrate Associated Microorganisms and Secondary Metabolite Production	p. 176
Macromarine Evolution	p. 176
Sponges	p. 177
Natural History of Sponges-a Primitive Phylum with Remarkable Biosynthetic Capabilities	p. 177
Molluscs	p. 186
Natural History of Molluscs-the Source of Numerous Preclinical Drug Leads	p. 186
Soft Corals	p. 189
Natural History of Cnidarians-the "Stinging Nettle" of the Sea	p. 189
Tunicates	p. 192
Natural History of Tunicates-Our Closest Marine Invertebrate Relations	p. 192
Conclusions	p. 194
References	p. 195
Microorganisms: Their Role in the Discovery and Development of Medicines
Introduction	p. 215
Bacteria	p. 218
Fungi	p. 220
Terrestrial and Marine Microorganisms	p. 221
Microbial Cultural Collection	p. 222
Evidence for "Uncultivable" Microbes	p. 223
Metagenomic Approach to Access Uncultivable Microbes	p. 224
Culturing Techniques to Produce Secondary Metabolites	p. 225
Evidence for New Biosynthetic Pathways in Known Microbes	p. 227
Genetic Pathway Engineering and Modulation of Post-translational Modification to Generate Novel Compounds	p. 227
Microbial Secondary Metabolits with Unique Biological Activity and Chemical Diversity	p. 228
Microbial Seconday Metabolites with Unique Pharmacological Activity	p. 231
Conclusions	p. 233
Structures Discussed in Tables 7.2 and 7.3	p. 233
References	p. 236
Advances in Technology
Advances in Biological Screening for Lead Discovery
Introduction	p. 245
Natural Product Screening and the Development of HTS	p. 247
Chapter Objectives	p. 247
Types of HTS Assays	p. 247
In vitro Biochemical Assays	p. 248
Cell-based Assays	p. 255
Modelling to Identify False Positives and Negatives	p. 261
Emerging Trends	p. 262
New HTS Approaches	p. 262
Acknowledgements	p. 265
References	p. 265
Advances in Instrumentation, Automation, Dereplication and Prefractionation
Introduction	p. 272
Dereplication	p. 274
Extraction	p. 275
Prefractio nation	p. 276
Isolation and Purification	p. 278
Automated Purification	p. 279
HPLC Separation Technologies	p. 279
Mass Spectrometry	p. 282
NMR	p. 285
Probe Technology	p. 285
Structure Elucidation	p. 287
Methods for Fast NMR	p. 288
Automated Structure Elucidation	p. 290
Configuration by NMR	p. 291
Residual Dipolar Couplings	p. 292
Conclusions	p. 292
References	p. 293
Natural Product Combinatorial Biosynthesis: Promises and Realities
Introduction	p. 299
A Brief History of Natural Product Biosynthesis	p. 300
Promises	p. 304
Realities	p. 307
Future Biotechnological Promises	p. 312
References	p. 314
Natural Products in Clinical Development
A Snapshot of Natural Product-Derived Compounds in Late Stage Clinical Development at the End of 2008
Introduction	p. 321
NP-derived Drugs Launched in the Last Five Years	p. 324
Late Stage NDAs and Clinical Candidates	p. 327
Antibacterial	p. 327
Oncology	p. 332
Other Therapeutic Areas	p. 340
Conclusions and Outlook	p. 342
References	p. 343
From Natural Product to Clinical Trials: NPI-0052 (Salinosporamide A), a Marine Actinomycete-Derived Anticancer Agent
Introduction	p. 355
Bioprospecting Marine Actinomycetes and the Discovery of Salinispora and NPI-0052	p. 355
The Ubiquitin-Proteasome, System as a Target for Drug Development	p. 356
Mechanism of Action	p. 358
Microbiology of Salinispora tropica, Fermentation and Scale-up	p. 359
Structural Biology and Structure-Activity Relation ship Studies	p. 361
Translational Biology	p. 363
IND-Enabling Studies of NPI-005	p. 364
API Manufacturing	p. 365
Formulation Development and Drug Product Manufacturing	p. 366
Pharmacodynamics	p. 367
Pharmacokinetics	p. 368
Clinical Trials	p. 368
Concluding Remarks	p. 370
Acknowledgements	p. 370
References	p. 370
From Natural Product to Clinical Trials: Bevirimat, a Plant-Derived Anti-AIDS Drug
Introduction	p. 374
Bioactivity-directed Fractionation and Isolation	p. 375
Lead Identification	p. 375
Lead Optimisation and SAR Study	p. 377
Modification of the BA Triterpene Skeleton	p. 377
Modification on C-3 Position of BA	p. 378
Introduction of C-28 Side Chain into BA	p. 382
Bifunctional BA Analogues-Potential for Maturation Inhibitor Development	p. 383
Mechanism of Action Studies of Bevirimat	p. 384
Preclinical Studies of Bevirimat	p. 385
Clinical Trials and Current Status of Bevirimat	p. 387
Conclusions	p. 388
Acknowledgements	p. 388
References	p. 388
Case Studies of Marketed Natural Product-derived Drugs
Daptomycin
Introduction	p. 395
Discovery of A21987C and Daptomycin	p. 396
Enzymatic Cleavage of the Fatty Acid Side Chain	p. 396
Chemical Modifications of the A21978C Core Peptide	p. 397
Biosynthesis	p. 397
Analysis of the Daptomycin Biosynthetic Gene Cluster	p. 397
Daptomycin Structure	p. 398
Mechanism of Action Studies	p. 399
Daptomycin Resistant Mutants	p. 400
Antibacterial Activities	p. 401
In vitro Activities	p. 401
In vivo Activities in Animal Models	p. 402
Clinical Studies	p. 402
Eli Lilly and Company	p. 402
The Passing of the Baton	p. 403
Cubist Pharmaceuticals	p. 403
Lessons Learned	p. 404
Epilogue	p. 405
References	p. 405
Micafungin
Introduction	p. 410
New Antifungal Compounds Discovered at Fujisawa (a Predecessor of Astellas Pharma Inc.)	p. 411
1,3-ß-Glucan Synthase Inhibition and Echinocandins	p. 413
From the Discovery of FR901379 to Clinical Studies of FK463 (Micafungin)	p. 414
Discovery of FR901379	p. 414
Generation of Lead Compound FR131535	p. 418
Lead Optimisation Leading to the Discovery FK463^12,13	p. 421
Preclinical Studies of FK463	p. 425
Industrial Manufacturing of Micafungin	p. 426
Clinical Studies of FK463	p. 426
Conclusions	p. 427
Acknowledgements	p. 427
References	p. 427
Subject Index
Table of Contents provided by Ingram. All Rights Reserved.

Natural Product Chemistry for Drug Discovery

At a Glance

Hardcover

Industry Reviews

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How to return your order

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