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A DNA‐Encoded Chemical Library Incorporating Elements of Natural Macrocycles
Author(s) -
Stress Cedric J.,
Sauter Basilius,
Schneider Lukas A.,
Sharpe Timothy,
Gillingham Dennis
Publication year - 2019
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.201902513
Subject(s) - natural (archaeology) , dna , computational biology , combinatorial chemistry , computer science , natural language processing , chemistry , genetics , biology , paleontology
Here we show 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 the custom synthesis of bifunctional building block libraries. This study outlines the importance of careful retrosynthetic design in DNA‐encoded libraries, while revealing areas where new DNA synthetic methods are needed.
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