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

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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

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Publication details

The article was received on 19 Sep 2018, accepted on 10 Oct 2018 and first published on 17 Oct 2018


Article type: Review Article
DOI: 10.1039/C8OB02327A
Citation: Org. Biomol. Chem., 2018, Advance Article
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    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., 2018, Advance Article , DOI: 10.1039/C8OB02327A

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