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The Effect of Vicinal Difluorination on the Conformation and Potency of Histone Deacetylase Inhibitors.
Ariawan, A Daryl; Mansour, Flora; Richardson, Nicole; Bhadbhade, Mohan; Ho, Junming; Hunter, Luke.
Afiliación
  • Ariawan AD; School of Chemistry, UNSW Sydney, Sydney, NSW 2052, Australia.
  • Mansour F; School of Chemistry, UNSW Sydney, Sydney, NSW 2052, Australia.
  • Richardson N; School of Chemistry, UNSW Sydney, Sydney, NSW 2052, Australia.
  • Bhadbhade M; Mark Wainwright Analytical Centre, UNSW Sydney, Sydney, NSW 2052, Australia.
  • Ho J; School of Chemistry, UNSW Sydney, Sydney, NSW 2052, Australia.
  • Hunter L; School of Chemistry, UNSW Sydney, Sydney, NSW 2052, Australia.
Molecules ; 26(13)2021 Jun 29.
Article en En | MEDLINE | ID: mdl-34209791
Histone deacetylase enzymes (HDACs) are potential targets for the treatment of cancer and other diseases, but it is challenging to design isoform-selective agents. In this work, we created new analogs of two established but non-selective HDAC inhibitors. We decorated the central linker chains of the molecules with specifically positioned fluorine atoms in order to control the molecular conformations. The fluorinated analogs were screened against a panel of 11 HDAC isoforms, and minor differences in isoform selectivity patterns were observed.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Inhibidores de Histona Desacetilasas / Histona Desacetilasas / Hidrocarburos Fluorados Límite: Humans Idioma: En Revista: Molecules Asunto de la revista: BIOLOGIA Año: 2021 Tipo del documento: Article País de afiliación: Australia Pais de publicación: Suiza
Texto completo
Añadir a Mi BVS
Imprimir
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Inhibidores de Histona Desacetilasas / Histona Desacetilasas / Hidrocarburos Fluorados Límite: Humans Idioma: En Revista: Molecules Asunto de la revista: BIOLOGIA Año: 2021 Tipo del documento: Article País de afiliación: Australia Pais de publicación: Suiza