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

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.

SUBMITTER: Luckhurst CA

PROVIDER: S-EPMC4716601 | biostudies-literature | 2016 Jan

REPOSITORIES: biostudies-literature

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

Luckhurst Christopher A CA Breccia Perla P Stott Andrew J AJ Aziz Omar O Birch Helen L HL Bürli Roland W RW Hughes Samantha J SJ Jarvis Rebecca E RE Lamers Marieke M Leonard Philip M PM Matthews Kim L KL McAllister George G Pollack Scott S Saville-Stones Elizabeth E Wishart Grant G Yates Dawn D Dominguez Celia C

ACS medicinal chemistry letters 20151210 1

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. ...[more]

PMID: 26819662

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