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Synthesis of a DNA-Encoded Macrocyclic Library Utilizing Intramolecular Benzimidazole Formation.
Chai, Jing; Arico-Muendel, Christopher C; Ding, Yun; Pollastri, Michael P; Scott, Sarah; Mantell, Mark A; Yao, Gang.
Afiliação
  • Chai J; Encoded Library Technologies/NCE Molecular Discovery, GSK, 200 Cambridge Park Drive, Cambridge, Massachusetts 02140, United States.
  • Arico-Muendel CC; Encoded Library Technologies/NCE Molecular Discovery, GSK, 200 Cambridge Park Drive, Cambridge, Massachusetts 02140, United States.
  • Ding Y; Encoded Library Technologies/NCE Molecular Discovery, GSK, 200 Cambridge Park Drive, Cambridge, Massachusetts 02140, United States.
  • Pollastri MP; Department of Chemistry and Chemical Biology, Northeastern University, Boston, Massachusetts 02115, United States.
  • Scott S; Encoded Library Technologies/NCE Molecular Discovery, GSK, 200 Cambridge Park Drive, Cambridge, Massachusetts 02140, United States.
  • Mantell MA; Encoded Library Technologies/NCE Molecular Discovery, GSK, 200 Cambridge Park Drive, Cambridge, Massachusetts 02140, United States.
  • Yao G; Encoded Library Technologies/NCE Molecular Discovery, GSK, 200 Cambridge Park Drive, Cambridge, Massachusetts 02140, United States.
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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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Compostos Macrocíclicos Idioma: En Ano de publicação: 2023 Tipo de documento: Article
Texto completo
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PubMed Links
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Compostos Macrocíclicos Idioma: En Ano de publicação: 2023 Tipo de documento: Article