655250-92-3Relevant academic research and scientific papers
MACROCYCLIC COMPOUNDS AND METHODS OF TREATMENT
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Page/Page column 43-44, (2016/04/26)
The instant invention describes macrocyclic compounds having therapeutic activity, and methods of treating disorders such as cancer, tumors and cell proliferation related disorders.
Evaluation of class i HDAC isoform selectivity of largazole analogues
Kim, Bumki,Park, Heekwang,Salvador, Lilibeth A.,Serrano, Patrick E.,Kwan, Jason C.,Zeller, Sabrina L.,Chen, Qi-Yin,Ryu, Soyoung,Liu, Yanxia,Byeon, Seongrim,Luesch, Hendrik,Hong, Jiyong
supporting information, p. 3728 - 3731 (2014/09/17)
Largazole is a potent class I selective histone deacetylase (HDAC) inhibitor. The majority of largazole analogues to date have modified the thiazole-thiazoline and the warhead moiety. In order to elucidate class I-specific structure-activity relationships, a series of analogues with modifications in the valine or the linker region were prepared and evaluated for their class I isoform selectivity. The inhibition profile showed that the C2 position of largazole has an optimal steric requirement for efficient HDAC inhibition and that substitution of the trans-alkene in the linker with an aromatic group results in complete loss of activity. This data will aid the design of class I isoform selective HDAC inhibitors.
