New Strategies Targeting Cancer Metabolism
Anticancer Drugs, Synthetic Analogues and Antitumor Agents
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New Strategies Targeting Cancer Metabolism: Anticancer Drugs, Synthetic Analogues and Antitumor Agents presents up-to-date synthetic strategies for three categories of antimetabolites: antifolates, purines and pyrimidines, the main classes of antimetabolites which are integrated into various pharmaceutical agents. Many of these antimetabolites are considered potent chemotherapeutic agents which have great potential impact on medical research. These main classes of antimetabolites are used in the treatment of critical diseases including cancer, malignancies, autoimmune diseases, and many other non-malignant diseases. Antineoplastic drugs such as alkylating agents which have significant effects are described. Novel synthetic strategies for many anticancer alkylating agents including nitrogen mustards, chlorambucil, melphalan, ifosamide, oxaliplatin and temozolomide are explored. Natural products have offered some of the most significant drugs for treating cancer, as many drugs currently in clinical use are derived from natural products as camptothecins, vinca alkaloids, and derivatives of podophyllotoxin. They provide a contribution that is essential for modern drug discovery and development. In this book, insights into a broad array of novel compounds are reviewed, well-recognized synthetic approaches are emphasized for further anticancer drug development and discovery, and the biological evaluation of novel synthesized compounds are included. This comprehensive reference is a valuable resource for medical chemists working in drug discovery and development, as well as pharmacologists and biochemists working in related fields.
Key Features
- Provides the only resource dedicated to synthetic strategies of antimetabolites
- Features synthetic strategies for nucleosides and their analogues
- Includes coverage of purine-, pyrimidine- and antifolate-based anticancer drugs
- The most significant anticancer alkylating agents and natural products are demonstrated
Readership
Organic and Medicinal Chemists working in drug discovery. Biochemists, pharmacologists
Table of Contents
- Cover image
- Title page
- Table of Contents
- Copyright
- Chapter 1: Medicinal chemistry of anticancer agents
- Abstract
- 1: Introduction
- 2: Biochemistry of nucleotide metabolism
- 3: Targets for chemotherapeutic agents and inhibition of biosynthetic pathways
- 4: Examples of antineoplastic agents
- References
- Chapter 2: Antifolate-based anticancer drugs
- Abstract
- 1: Introduction
- 2: Classical antifolate drugs (polyglutamate antifolate)
- 3: Nonclassical antifolate drugs (nonpolyglutamable antifolates)
- References
- Chapter 3: Purine-based anticancer drugs
- Abstract
- 1: Introduction
- 2: Mercaptopurine drug
- 3: 6-Thioguanine
- 4: Azathioprine
- 5: Pentostatin
- 6: Cladribine
- 7: Fludarabine phosphate
- 8: Clofarabine
- 9: Nelarabine
- References
- Chapter 4: Pyrimidine-based anticancer drugs
- Abstract
- 1: Introduction
- 2: Cytosine analogs
- 3: Uracil analogs
- References
- Chapter 5: Synthetic strategies for anticancer antifolates
- Abstract
- 1: Introduction
- 2: Classical antifolates: Syntheses and biological evaluation
- 3: Nonclassical antifolates: Syntheses and biological evaluation
- References
- Chapter 6: Synthetic strategies for purine nucleoside analogs
- Abstract
- 1: Introduction
- 2: Examples of potent anticancer purine nucleoside analogs
- 3: Nucleoside analogs: Syntheses and biological evaluation
- References
- Chapter 7: Synthetic strategies for pyrimidine nucleoside analogs
- Abstract
- 1: Introduction
- 2: Examples of potent anticancer pyrimidine nucleoside analogs
- 3: Nucleoside analogs: Syntheses and biological evaluations
- References
- Chapter 8: Anticancer alkylating agents
- Abstract
- 1: Introduction
- 2: Nitrogen mustards
- 3: Aziridines
- 4: Epoxides
- 5: Methanesulfonates
- 6: Nitrosoureas
- 7: Triazenes
- 8: Methylhydrazines
- 9: 1,3,5-Triazines: Hexamethylmelamine and trimetelamol
- 10: Platinum complexes
- 11: Examples of potent anticancer alkylating agents
- 12: Synthetic strategies and biological evaluations
- References
- Chapter 9: Natural products in chemotherapy of cancers
- Abstract
- 1: Introduction
- 2: Podophyllotoxins
- 3: Vinca alkaloids
- 4: Camptothecin (CPT)
- 5: Paclitaxel
- 6: Epothilones
- 7: Dolastatin
- 8: Eribulin (E7389)
- References
- Chapter 10: Synthetic strategies for antimetabolite analogs in our laboratory
- Abstract
- 1: Introduction
- 2: Synthesis of antifolate analogs
- 3: Synthesis of mercaptopurine antimetabolite analogs
- 4: Pyrimidine and heterocyclic thioglycosides
- 5: Pyrimidine and pyridine N-non-nucleoside analogs
- References
- Index
Product details
- No. of pages: 628
- Language: English
- Copyright: © Elsevier 2022
- Published: May 17, 2022
- Imprint: Elsevier
- Paperback ISBN: 9780128217832
- eBook ISBN: 9780128217849
About the Authors
Galal Elgemeie
Galal H. Elgemeie is the author of over 270 scientific international papers on heterocyclic chemistry and medicinal chemistry. His research interests include the development and mechanistic understanding of organic reactions and their application to the synthesis of antimetabolic agents. He was an international elected member of the Scientific Board of the International Basic Sciences Programme (IBSP), UNESCO, in Paris, France. He was a postdoctoral fellow of the Alexander von Humboldt Foundation in Germany, the Fulbright in USA, the British Council in England, and then the German Research Foundation (DFG) in Germany. He supervised several cooperation projects with the European Community under the TEMUPS programme, Prof. Elgemeie was nominated as one of the leading scientists of the COMSTECH in the year 2009 Report. Prof. Elgemeie's research activities have received many awards including The African Union Scientific Award "Continental Scientific Award" in Science and Technology, The ISESCO Scientific Award and The Egypt State Honor Award "NILE", among many others.
Affiliations and Expertise
Department of Chemistry, Helwan University, Cairo, Egypt
Reham Mohamed-Ezzat
Reham A. Mohamed-Ezzat is a researcher in the Chemistry of Natural and Microbial Products Department, Pharmaceutical & Drug Industries Research Division, National Research Center in Egypt. She got her B.Sc (2010) in Chemistry & Biochemistry-Faculty of Science. She was awarded her M.Sc. (2015) & PhD degree of science in organic chemistry in 2019 from Helwan University. She has published many books and articles in international journals in the field of bioorganic and medicinal chemistry. She has extensive experience in the field of design and synthesis of novel molecules of medicinal application, as well as the implementation of new strategies in the syntheses of bioactive compounds.
Affiliations and Expertise
Chemistry of Natural and Microbial Products Department, National Research Center, Cairo, Egypt
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