Back to Search Start Over

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

Authors :
Luckhurst CA
Breccia P
Stott AJ
Aziz O
Birch HL
Bürli RW
Hughes SJ
Jarvis RE
Lamers M
Leonard PM
Matthews KL
McAllister G
Pollack S
Saville-Stones E
Wishart G
Yates D
Dominguez C
Source :
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).
Publication Year :
2015

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.

Details

Language :
English
ISSN :
1948-5875
Volume :
7
Issue :
1
Database :
MEDLINE
Journal :
ACS medicinal chemistry letters
Publication Type :
Academic Journal
Accession number :
26819662
Full Text :
https://doi.org/10.1021/acsmedchemlett.5b00302