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ID: ALA3792315

Journal: ACS Med Chem Lett

Title: 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.

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.

CiteXplore: 26819662

DOI: 10.1021/acsmedchemlett.5b00302