Potent, Selective, and CNS-Penetrant Tetrasubstituted Cyclopropane Class IIa Histone Deacetylase (HDAC) Inhibitors.

Autor:	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.
Jazyk:	angličtina
Zdroj:	ACS medicinal chemistry letters [ACS Med Chem Lett] 2015 Dec 10; Vol. 7 (1), pp. 34-9. Date of Electronic Publication: 2015 Dec 10 (Print Publication: 2016).
DOI:	10.1021/acsmedchemlett.5b00302
Abstrakt:	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.
Databáze:	MEDLINE
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