Discovery of macrocyclic HDACs 1, 2, and 3 selective inhibitors for HIV latency reactivation.

Basic Information

ID: ALA4811291

Journal: Bioorg Med Chem Lett

Title: Discovery of macrocyclic HDACs 1, 2, and 3 selective inhibitors for HIV latency reactivation.

Authors: Yu W, Fells J, Clausen D, Liu J, Klein DJ, Christine Chung C, Myers RW, Wu J, Wu G, Howell BJ, Barnard RJO, Kozlowski J.

Abstract: A series of unique macrocyclic HDACs 1, 2, and 3 selective inhibitors were identified with good enzymatic activity and high selectivity over HDACs 6 and 8. These macrocyclic HDAC inhibitors used an ethyl ketone as the zinc-binding group. Compounds 25 and 26 stood out as leads due to their low double-digit nM EC₅₀s in the 2C4 cell-based HIV latency reactivation assay. The PK profiles of these macrocyclic HDAC inhibitors still needed improvement.

CiteXplore: 34091041

DOI: 10.1016/j.bmcl.2021.128168

Patent ID: ┄

Associated Items: Associated Bioactivities Associated Assays Associated Compounds Associated Targets