New Strategies Targeting Cancer Metabolism

Anticancer Drugs, Synthetic Analogues and Antitumor Agents

1st Edition - May 17, 2022
Imprint: Elsevier
Authors: Galal H. Elgemeie, Reham A. Mohamed-Ezzat
Language: English
Paperback ISBN:
9 7 8 - 0 - 1 2 - 8 2 1 7 8 3 - 2
eBook ISBN:
9 7 8 - 0 - 1 2 - 8 2 1 7 8 4 - 9

New Strategies Targeting Cancer Metabolism: Anticancer Drugs, Synthetic Analogues and Antitumor Agents presents up-to-date synthetic strategies for three categories of antimetab… Read more

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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.

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

Galal H. 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 A. 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

Life Sciences

Physical Sciences & Engineering

Social Sciences & Humanities

Health