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Enantioselective synthesis of adamantylalanine and carboranylalanine and their incorporation into the proteasome inhibitor bortezomib.
de Bruin, Gerjan; Mock, Elliot D; Hoogendoorn, Sascha; van den Nieuwendijk, Adrianus M C H; Mazurek, Jaroslaw; van der Marel, Gijsbert A; Florea, Bogdan I; Overkleeft, Herman S.
Afiliação
  • de Bruin G; Leiden Institute of Chemistry, Leiden University, Einsteinweg 55, 2333 CC Leiden, The Netherlands. h.s.overkleeft@lic.leidenuniv.nl.
  • Mock ED; Leiden Institute of Chemistry, Leiden University, Einsteinweg 55, 2333 CC Leiden, The Netherlands. h.s.overkleeft@lic.leidenuniv.nl.
  • Hoogendoorn S; Leiden Institute of Chemistry, Leiden University, Einsteinweg 55, 2333 CC Leiden, The Netherlands. h.s.overkleeft@lic.leidenuniv.nl.
  • van den Nieuwendijk AM; Leiden Institute of Chemistry, Leiden University, Einsteinweg 55, 2333 CC Leiden, The Netherlands. h.s.overkleeft@lic.leidenuniv.nl.
  • Mazurek J; Crystallics B.V., Meibergdreef 31, 1105 AZ Amsterdam, The Netherlands.
  • van der Marel GA; Leiden Institute of Chemistry, Leiden University, Einsteinweg 55, 2333 CC Leiden, The Netherlands. h.s.overkleeft@lic.leidenuniv.nl.
  • Florea BI; Leiden Institute of Chemistry, Leiden University, Einsteinweg 55, 2333 CC Leiden, The Netherlands. h.s.overkleeft@lic.leidenuniv.nl.
  • Overkleeft HS; Leiden Institute of Chemistry, Leiden University, Einsteinweg 55, 2333 CC Leiden, The Netherlands. h.s.overkleeft@lic.leidenuniv.nl.
Chem Commun (Camb) ; 52(21): 4064-7, 2016 Mar 14.
Article em En | MEDLINE | ID: mdl-26894389
ABSTRACT
The incorporation of adamantylalanine and carboranylalanine at the P2 site of bortezomib is well tolerated and provided potent cell permeable proteasome inhibitors with increased off-rates compared to bortezomib. Adamantylalanine and carboranylalanine were synthesized enantioselectively by an asymmetric Strecker reaction on Ellmans tert-butyl sulfinimines.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Fenilalanina / Compostos de Boro / Adamantano / Complexo de Endopeptidases do Proteassoma / Inibidores de Proteassoma / Bortezomib Limite: Humans Idioma: En Ano de publicação: 2016 Tipo de documento: Article
Texto completo
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XML
PubMed Links
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Fenilalanina / Compostos de Boro / Adamantano / Complexo de Endopeptidases do Proteassoma / Inibidores de Proteassoma / Bortezomib Limite: Humans Idioma: En Ano de publicação: 2016 Tipo de documento: Article