Enediynes are natural products with highly active cytotoxicity and antibacterial activity, and thus have significant potential in the development of anti-cancer treatments. However, they are not readily available and can degrade rapidly during isolation; one solution is to produce them using total synthesis.
Dynemicin A and uncialamycin are two such enediynes, with similar structures, for which total synthesis has been achieved. This book presents the isolation and preparation of these two compounds and their analogues through various synthesis strategies. Details of the structural elements essential to their anti-cancer activity are presented, with the objective of explaining and optimizing their biological activities and potential development as drugs.
- Presents two natural ènediynes with similar structures whose total syntheses have been accomplished
- Explores structural analogs of preparation for purposes of optimizing the anti-cancer activity
- Describes the total syntheses of dynemicin A, the uncialamycine, as well as analogs by emphasizing the synthesis strategies adopted
- Features studies of the biological activities and data to bring out the structural elements of these essential compounds
Undergraduate and graduate students in chemistry studying medicinal chemistry or pharmaceutical chemistry; research chemists and biochemists working in pharmaceutical and biotechnology industries
- 1: Dynemicin A
- 1.1 Isolation and characterization
- 1.2 Biosynthesis
- 1.3 Total synthesis, analogues and biological activities
- 2: Uncialamycin
- 2.1 Isolation and characterization
- 2.2 Biosynthesis
- 2.3 Total synthesis and analogues
- No. of pages:
- © ISTE Press - Elsevier 2016
- 14th June 2016
- ISTE Press - Elsevier
- eBook ISBN:
- Hardcover ISBN:
Daniel Best is a postdoctoral researcher at the University of Rennes 1 in France. He is currently developing the synthesis of uncialamycin analogues.
Postdoctoral Researcher, Université de Rennes, France
Mickael Jean is Associate Professor at the University of Rennes 1 in France. His research is concerned with the challenges of total synthesis of natural products and the development of anti-cancer medical chemistry programs.
Lecturer, University of Rennes 1, France
Pierre van de Weghe is Professor in organic chemistry at the University of Rennes 1 in France. His work focuses on the total synthesis of natural products and analogues, as well as research into new components in anti-cancer activity..
University of Rennes 1, France