Issue 7, 2019

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

Abstract

Diversity-oriented synthesis has historically focused on the generation of small-molecule collections with considerable scaffold, stereochemical, and appendage diversity. Recently, this focus has begun to shift to the production of small-molecule libraries with diverse biological activities. It is currently not clear which properties and structural features of molecules are predictive of diverse performance in biological assays, and a better understanding of this relationship is critical for the development of performance-diverse small-molecule libraries for the discovery of novel probes for challenging targets. This review explores recent synthetic strategies for the production of bioactive small molecules and concludes with a presentation of current methods that enable the assessment of the biological performance diversity of small-molecule libraries.

Graphical abstract: Next generation diversity-oriented synthesis: a paradigm shift from chemical diversity to biological diversity

Article information

Article type
Review Article
Submitted
19 sep 2018
Accepted
10 okt 2018
First published
17 okt 2018

Org. Biomol. Chem., 2019,17, 1608-1623

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

I. Pavlinov, E. M. Gerlach and L. N. Aldrich, Org. Biomol. Chem., 2019, 17, 1608 DOI: 10.1039/C8OB02327A

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