title: Capturing Biological Activity in Natural Product Fragments by Chemical Synthesis.
abstract: Natural products have had an immense influence on science and have directly led to the introduction of many drugs. Organic chemistry, and its unique ability to tailor natural products through synthesis, provides an extraordinary approach to unlock the full potential of natural products. In this Review, an approach based on natural product derived fragments is presented that can successfully address some of the current challenges in drug discovery. These fragments often display significantly reduced molecular weights, reduced structural complexity, a reduced number of synthetic steps, while retaining or even improving key biological parameters such as potency or selectivity. Examples from various stages of the drug development process up to the clinic are presented. In addition, this process can be leveraged by recent developments such as genome mining, antibody-drug conjugates, and computational approaches. All these concepts have the potential to identify the next generation of drug candidates inspired by natural products.
authors.affiliation: Department of Chemistry, University of Basel, Switzerland.
authors.forename: Erika A
authors.initials: EA
authors.lastname: Crane
authors.affiliation: Department of Chemistry, University of Basel, Switzerland. karl.gademann@uzh.ch.|Department of Chemistry, University of Zürich, Winterthurerstrasse 190, CH-8057, Zürich, Switzerland. karl.gademann@uzh.ch.
authors.forename: Karl
authors.identifier: http://orcid.org/0000-0003-3053-0689
authors.initials: K
authors.lastname: Gademann
mesh_terms: D000818:Animals; D001688:Biological Products / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D055808:Drug Discovery; D006801:Humans
chemical_list: D001688:Biological Products
keywords: drug discovery; medicinal chemistry; natural products; organic chemistry; organic synthesis
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