Synthesis of a DNA-Encoded Macrocyclic Library Utilizing Intramolecular Benzimidazole Formation.
Bioconjug Chem
; 34(6): 988-993, 2023 06 21.
Article
em En
| MEDLINE
| ID: mdl-37216465
ABSTRACT
Macrocycles occupy chemical space "beyond the rule of five". They bridge traditional bioactive small molecule drugs and macromolecules and have the potential to modulate challenging targets such as PPI or proteases. Here we report an on-DNA macrocyclization reaction utilizing intramolecular benzimidazole formation. A 129-million-member macrocyclic library composed of a privileged benzimidazole core, a dipeptide sequence (natural or non-natural), and linkers of varying length and flexibility was designed and synthesized.
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1
Base de dados:
MEDLINE
Assunto principal:
Compostos Macrocíclicos
Idioma:
En
Ano de publicação:
2023
Tipo de documento:
Article