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1. Synthesis and direct assay of large macrocycle diversities by combinatorial late-stage modification at picomole scale

Author

Sevan Habeshian, Manuel Leonardo Merz, Gontran Sangouard, Ganesh Kumar Mothukuri, Mischa Schüttel, Zsolt Bognár, Cristina Díaz-Perlas, Jonathan Vesin, Julien Bortoli Chapalay, Gerardo Turcatti, Laura Cendron, Alessandro Angelini, and Christian Heinis

Subjects
Science
Abstract

Macrocycles have potential as therapeutics, but their libraries are currently not large enough for high-throughput screening. Here, the authors show a combinatorial approach to generate a library of almost 20’000 macrocycles by conjugating carboxylic-acid fragments to macrocyclic scaffolds, identifying nanomolar inhibitors against thrombin and binders of MDM2.

Published
2022
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