Multiple Chemical Features Impact Biological Performance Diversity of a Highly Active Natural Product‐Inspired Library

RS Hippman, I Pavlinov, Q Gao… - …, 2020 - Wiley Online Library
A systematic, diversity‐oriented synthesis approach was employed to access a natural
product‐inspired flavonoid library with diverse chemical features, including chemical …

Next generation diversity-oriented synthesis: A paradigm shift from chemical diversity to biological diversity

I Pavlinov, EM Gerlach, LN Aldrich - Organic & Biomolecular Chemistry, 2019 - pubs.rsc.org
Diversity-oriented synthesis has historically focused on the generation of small-molecule
collections with considerable scaffold, stereochemical, and appendage diversity. Recently …

Advancing chemistry and biology through diversity-oriented synthesis of natural product-like libraries

S Shang, DS Tan - Current opinion in chemical biology, 2005 - Elsevier
Natural products provide the inspiration for a variety of strategies used in the diversity-
oriented synthesis of novel small-molecule libraries. These libraries can be based on core …

Systematic diversity-oriented synthesis of reduced flavones from γ-pyrones to probe biological performance diversity

EM Gerlach, MA Korkmaz, I Pavlinov, Q Gao… - ACS Chemical …, 2019 - ACS Publications
Diversity-oriented synthesis (DOS) has historically focused on the development of small-
molecule collections with considerable chemical diversity with the hypothesis that chemical …

Integration of high-content screening and untargeted metabolomics for comprehensive functional annotation of natural product libraries

KL Kurita, E Glassey… - Proceedings of the …, 2015 - National Acad Sciences
Traditional natural products discovery using a combination of live/dead screening followed
by iterative bioassay-guided fractionation affords no information about compound structure …

Canvass: A crowd-sourced, natural-product screening library for exploring biological space

SE Kearney, G Zahoránszky-Kőhalmi… - ACS central …, 2018 - ACS Publications
Natural products and their derivatives continue to be wellsprings of nascent therapeutic
potential. However, many laboratories have limited resources for biological evaluation …

Using biological performance similarity to inform disaccharide library design

T Tanikawa, M Fridman, W Zhu, B Faulk… - Journal of the …, 2009 - ACS Publications
Designing better small-molecule discovery libraries requires having methods to assess the
consequences of different synthesis decisions on the biological performance of resulting …

Strategies to diversify natural products for drug discovery

G Li, HX Lou - Medicinal research reviews, 2018 - Wiley Online Library
Natural product libraries contain specialized metabolites derived from plants, animals, and
microorganisms that play a pivotal role in drug discovery due to their immense structural …

Expanding the range of 'druggable'targets with natural product-based libraries: an academic perspective

RA Bauer, JM Wurst, DS Tan - Current opinion in chemical biology, 2010 - Elsevier
Existing drugs address a relatively narrow range of biological targets. As a result, libraries of
drug-like molecules have proven ineffective against a variety of challenging targets, such as …

Building natural product libraries using quantitative clade-based and chemical clustering strategies

VM Anderson, KL Wendt, FZ Najar, LI McCall… - Msystems, 2021 - Am Soc Microbiol
The success of natural product-based drug discovery is predicated on having chemical
collections that offer broad coverage of metabolite diversity. We propose a simple set of tools …