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Potent, Selective, and CNS-Penetrant Tetrasubstituted Cyclopropane Class IIa Histone Deacetylase (HDAC) Inhibitors.
Luckhurst, Christopher A; Breccia, Perla; Stott, Andrew J; Aziz, Omar; Birch, Helen L; Bürli, Roland W; Hughes, Samantha J; Jarvis, Rebecca E; Lamers, Marieke; Leonard, Philip M; Matthews, Kim L; McAllister, George; Pollack, Scott; Saville-Stones, Elizabeth; Wishart, Grant; Yates, Dawn; Dominguez, Celia.
Afiliação
  • Luckhurst CA; BioFocus, Charles River , Chesterford Research Park, Saffron Walden, Essex, CB10 1XL, United Kingdom.
  • Breccia P; BioFocus, Charles River , Chesterford Research Park, Saffron Walden, Essex, CB10 1XL, United Kingdom.
  • Stott AJ; BioFocus, Charles River , Chesterford Research Park, Saffron Walden, Essex, CB10 1XL, United Kingdom.
  • Aziz O; BioFocus, Charles River , Chesterford Research Park, Saffron Walden, Essex, CB10 1XL, United Kingdom.
  • Birch HL; BioFocus, Charles River , Chesterford Research Park, Saffron Walden, Essex, CB10 1XL, United Kingdom.
  • Bürli RW; BioFocus, Charles River , Chesterford Research Park, Saffron Walden, Essex, CB10 1XL, United Kingdom.
  • Hughes SJ; BioFocus, Charles River , Chesterford Research Park, Saffron Walden, Essex, CB10 1XL, United Kingdom.
  • Jarvis RE; BioFocus, Charles River , Chesterford Research Park, Saffron Walden, Essex, CB10 1XL, United Kingdom.
  • Lamers M; BioFocus, Charles River , Chesterford Research Park, Saffron Walden, Essex, CB10 1XL, United Kingdom.
  • Leonard PM; BioFocus, Charles River , Chesterford Research Park, Saffron Walden, Essex, CB10 1XL, United Kingdom.
  • Matthews KL; BioFocus, Charles River , Chesterford Research Park, Saffron Walden, Essex, CB10 1XL, United Kingdom.
  • McAllister G; BioFocus, Charles River , Chesterford Research Park, Saffron Walden, Essex, CB10 1XL, United Kingdom.
  • Pollack S; BioFocus, Charles River , Chesterford Research Park, Saffron Walden, Essex, CB10 1XL, United Kingdom.
  • Saville-Stones E; BioFocus, Charles River , Chesterford Research Park, Saffron Walden, Essex, CB10 1XL, United Kingdom.
  • Wishart G; BioFocus, Charles River , Chesterford Research Park, Saffron Walden, Essex, CB10 1XL, United Kingdom.
  • Yates D; BioFocus, Charles River , Chesterford Research Park, Saffron Walden, Essex, CB10 1XL, United Kingdom.
  • Dominguez C; CHDI Management/CHDI Foundation Inc. , 6080 Center Drive, Suite 100, Los Angeles, California 90045, United States.
ACS Med Chem Lett ; 7(1): 34-9, 2016 Jan 14.
Article em En | MEDLINE | ID: mdl-26819662
ABSTRACT
Potent and selective class IIa HDAC tetrasubstituted cyclopropane hydroxamic acid inhibitors were identified with high oral bioavailability that exhibited good brain and muscle exposure. Compound 14 displayed suitable properties for assessment of the impact of class IIa HDAC catalytic site inhibition in preclinical disease models.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Idioma: En Ano de publicação: 2016 Tipo de documento: Article
Texto completo
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PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Idioma: En Ano de publicação: 2016 Tipo de documento: Article