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

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• 作者：Christopher A. Luckhurst ; Perla Breccia ; Andrew J. Stott ; Omar Aziz ; Helen L. Birch ; Roland W. Bürli ; Samantha J. Hughes ; Rebecca E. Jarvis ; Marieke Lamers ; Philip M. Leonard ; Kim L. Matthews ; George McAllister ; Scott Pollack ; Elizabeth Saville-Stones ; Grant Wishart ; Dawn Yates ; Celia Dominguez
• 刊名：ACS Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：January 14, 2016
• 年：2016
• 卷：7
• 期：1
• 页码：34-39
• 全文大小：404K
• ISSN：1948-5875

文摘

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.