Description
Book SynopsisThis book offers an integrated review of the most recent trends in natural products drug discovery and key lead candidates that are outstanding for their chemistry and biology as a starting point in novel drug development. The authors focus on different trends that are and will continue to be impacting multiples stages of modern drug discovery from NPs that have not been included in other works. This is complemented with a series of case studies from leading experts from industry and academia on key molecules and derivatives that have been chosen for their novelty in chemistry, biology and clinical applications. The book intends to reflect the current confluence of different disciplines in chemical biology and synthetic chemistry supported by a more profound knowledge of systems biology that ensures the concurrency and synergisms of expertise from different research fields that impact in the discovery of novel molecules. In the first section the chapters reflect recent approaches to exploit the biosynthetic potential of microbial resources (including genome mining, metagenomic and epigenetic approaches), as well as biosynthetic chemistry tools to respond to product supply and novel screening alternatives that have lead to the discovery of novel chemistry. The second part reviews, in the form of case studies, some examples of bioactive molecules in the important therapeutic areas of antiinfectives, oncology and antiparasitics.
Trade Review"The book covers a wide range of topics concerning natural products,especially their discovery, synthesis and biological activities relevant for drug discovery." "It is interesting for chemists to get a general overview of recently discovered natural products as potential synthetic targets as well as for biochemists/biologists as a basis for further genetically driven discoveries.Pharmacologists and researchers in medicine may get an inspiration pursuing further testing of the compounds shown or similar ones from the same classes." -- Dr. Sabine Amslinger, University of Regensburg (Germany) * ChemMedChem 2013, 8, 1415 – 1418 *
Table of ContentsIntroduction; Part one: Semisynthesis/ synthesis de novo of NPs: Semisynthesis approach of Ecteinascidin 743 (ET-743, Yondelis«); Chondramides and Chivosazoles - Two metabolites which interfere with the actin cytoskeleton; Class III lantibiotics - an emerging family of thioether containing peptidesMutant manufacturers; progress in enhancing the neurotrophic effects of natural FKBP ligands; Part two: Engineering NP synthetic pathways and genome mining: biosynthesis of indolocarbazole alkaloids and generation of novel derivatives by combinatorial biosynthesis; new lantibiotics from natural and engineered strains; mining microbial genomes for metabolic products of cryptic pathways; mining cyanobacterial genomes for drug-like and bioactive natural products; pigenetic approaches to natural product synthesis in fungi; Part three: New methodologies and screening technologies for the exploitation of microbial resources: novel approaches for exploiting microbial resources at Fundacion MEDINA; discovery and development of Platensimycin and Platencin; coupling chemical genomics and natural products: the discovery of parnafungins and novel antifungal leads; Part four: Novel microbial natural products and derivatives: Retapamulin-a first-in-class pleuromutilin antibiotic; natural products: new agents against MDR tuberculosis; the contribution of marine chemistry in the field of antimalarial research; epothilones as lead structures for new anticancer drugs; future challenges.
