1126530-16-2Relevant academic research and scientific papers
METHOD FOR PREPARING LARGAZOLE ANALOGS AND USES THEREOF
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Paragraph 00368, (2016/09/26)
Analogs of largazole are described herein. Methods of treating cancer and blood disorders using largazole and largazole analogs and pharmaceutical compositions comprising the same are additionally described herein. Methods for preparing largazole analogs are likewise described.
Modular synthesis and biological activity of pyridyl-based analogs of the potent Class i Histone Deacetylase Inhibitor Largazole
Clausen, Dane J.,Smith, William B.,Haines, Brandon E.,Wiest, Olaf,Bradner, James E.,Williams, Robert M.
, p. 5061 - 5074 (2015/08/03)
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.
Synthesis and conformation#activity relationships of the peptide isosteres of FK228 and largazole
Bowers, Albert A.,Greshook, Thomas J.,West, Nathan,Estiu, Guillermina,Schreiber, Stuart L.,et al.
supporting information; experimental part, p. 2900 - 2905 (2009/07/30)
The peptide isosteres (10 and 11) of the naturally occurring and potent histone deacetylase (HDAC) Inhibitors FK228 and largazole have been synthesized and evaluated side-by-side with FK228, largazole, and SAHA for inhibition of the class I HDACs 1, 2, 3,
