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A DNA-Encoded Macrocycle Library that Resembles Natural Macrocycles

preprint
submitted on 06.02.2019 and posted on 06.02.2019 by Cedric Stress, Basilius Sauter, Lukas A. Schneider, Timothy Sharpe, Dennis G. Gillingham

Herein we perform a seven-step chemical synthesis of a DNA-encoded macrocycle library (DEML) on DNA. Inspired by polyketide and mixed peptide-polyketide natural products, the library was designed to incorporate rich backbone diversity. Achieving this diversity, however, comes at the cost of custom synthesis of bifunctional building block libraries. Our work outlines the importance of careful retrosynthetic design in DNA-encoded libraries, while revealing areas where new DNA synthetic methods are needed.

History

Email Address of Submitting Author

cedric.stress@unibas.ch

Institution

University of Basel

Country

Switzerland

ORCID For Submitting Author

0000-0002-6880-7498

Declaration of Conflict of Interest

No conflict of interest

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Read the published paper

in Angewandte Chemie International Edition

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