Chapter One
THE CHEMISTRY AND BIOLOGY
OFEPOTHILONES-LEADSTRUCTURES
FOR THE DISCOVERY OF IMPROVED
MICROTUBULE INHIBITORS
Karl-Heinz Altmann
Department of Chemistry and Applied BioSciences, Institute of Pharmaceutical Sciences,
Swiss Federal Institute of Technology (ETH), Zürich, Switzerland
1.1 INTRODUCTION
Cancer represents one of the most severe health problems worldwide, and the development
of new anticancer drugs and more effective treatment strategies are fields
of utmost importance in drug discovery and clinical therapy. Much of the research
in these areas is currently focused on cancer-specific mechanisms and the corresponding
molecular targets (e.g., kinases related to cell cycle progression or signal
transduction), but the search for improved cytotoxic agents (acting on ubiquitous
targets such as DNA or tubulin) still constitutes an important part of modern anticancer
drug discovery. As the major types of solid human tumors (breast, lung,
prostate, and colon), which represent most cancer cases today, are multicausal in
nature, there is a growing recognition that the ... read full excerpt from Medicinal Chemistry of Bioactive Natural Products ebook
