Modular synthesis and biological activity of pyridyl-based analogs of the potent Class I Histone Deacetylase Inhibitor Largazole.

Basic Information

ID: ALA3593208

Journal: Bioorg Med Chem

Title: Modular synthesis and biological activity of pyridyl-based analogs of the potent Class I Histone Deacetylase Inhibitor Largazole.

Authors: Clausen DJ, Smith WB, Haines BE, Wiest O, Bradner JE, Williams RM.

Abstract: The formation of a series of analogs containing a pyridine moiety in place of the natural thiazole heterocycle, based on the potent, naturally occurring HDAC inhibitor Largazole has been accomplished. The synthetic strategy was designed modularly to access multiple inhibitors with different aryl functionalities containing both the natural depsipeptide and peptide isostere variant of the macrocycle. The cytotoxicity and biochemical activity of the library of HDAC inhibitors is described herein.

CiteXplore: 26054247

DOI: 10.1016/j.bmc.2015.03.063

Patent ID: