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

ACS Medicinal Chemistry Letters
Christopher A LuckhurstCelia Dominguez

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.

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Citations

Jul 23, 2016·Cell Chemical Biology·Alex R MaolanonChristian A Olsen
Dec 7, 2016·Chemistry : a European Journal·Christian MeynersFranz-Josef Meyer-Almes
May 31, 2019·Physical Chemistry Chemical Physics : PCCP·Huawei LiuRuibo Wu
Feb 28, 2020·Nature Communications·Son HoangPu-Xian Gao
Oct 20, 2018·Current Medicinal Chemistry·Loredana CappellacciRiccardo Petrelli
Jan 5, 2020·Journal of Biomolecular Structure & Dynamics·Kriti Kashyap, Rita Kakkar
Jan 8, 2020·International Journal of Molecular Sciences·Shana V StoddardDavita L Watkins
Feb 12, 2021·Journal of Medicinal Chemistry·Jeffrey Y W MakDavid P Fairlie
Jan 12, 2021·ChemMedChem·Jelena MelesinaWolfgang Sippl
Mar 20, 2021·ACS Medicinal Chemistry Letters·Andrew J StottCelia Dominguez
Jul 2, 2020·Journal of Medicinal Chemistry·Terence C S HoA Ganesan
Oct 24, 2020·Journal of Medicinal Chemistry·Giuseppe Felice MangiatordiMarialessandra Contino

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