Header

UZH-Logo

Maintenance Infos

Capturing biological activity in natural product fragments by chemical synthesis


Crane, Erika A; Gademann, Karl (2016). Capturing biological activity in natural product fragments by chemical synthesis. Angewandte Chemie Internationale Edition, 55(12):3882-3902.

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.

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.

Statistics

Citations

26 citations in Web of Science®
26 citations in Scopus®
Google Scholar™

Altmetrics

Downloads

18 downloads since deposited on 02 Jun 2016
14 downloads since 12 months
Detailed statistics

Additional indexing

Item Type:Journal Article, refereed, further contribution
Communities & Collections:07 Faculty of Science > Department of Chemistry
Dewey Decimal Classification:540 Chemistry
Language:English
Date:2016
Deposited On:02 Jun 2016 14:09
Last Modified:08 Dec 2017 19:35
Publisher:Wiley-VCH Verlag
ISSN:1433-7851
Free access at:Publisher DOI. An embargo period may apply.
Publisher DOI:https://doi.org/10.1002/anie.201505863

Download

Download PDF  'Capturing biological activity in natural product fragments by chemical synthesis'.
Preview
Content: Published Version
Filetype: PDF (http://creativecommons.org/licenses/by-nc/4.0/)
Size: 9MB
View at publisher
Licence: Creative Commons: Attribution-NonCommercial 4.0 International (CC BY-NC 4.0)