944457-57-2Relevant academic research and scientific papers
A series of potent and selective, triazolylphenyl-based histone deacetylases inhibitors with activity against pancreatic cancer cells and Plasmodium falciparum
Chen, Yufeng,Lopez-Sanchez, Miriam,Savoy, Doris N.,Billadeau, Daniel D.,Dow, Geoffrey S.,Kozikowski, Alan P.
supporting information; scheme or table, p. 3437 - 3448 (2009/04/07)
The discovery of the rules governing the inhibition of the various HDAC isoforms is likely to be key to identifying improved therapeutics that act as epigenetic modulators of gene transcription. Herein we present results on the modification of the CAP reg
Functional differences in epigenetic modulators - Superiority of mercaptoacetamide-based histone deacetylase inhibitors relative to hydroxamates in cortical neuron neuroprotection studies
Kozikowski, Alan P.,Chen, Yufeng,Gaysin, Arsen,Chen, Bin,D'Annibale, Melissa A.,Suto, Carla M.,Langley, Brett C.
, p. 3054 - 3061 (2008/02/09)
We compare the ability of two structurally different classes of epigenetic modulators, namely, histone deacetylase (HDAC) inhibitors containing either a hydroxamate or a mercaptoacetamide as the zinc binding group, to protect cortical neurons in culture from oxidative stress-induced death. This study reveals that some of the mercaptoacetamide-based HDAC inhibitors are fully protective, whereas the hydroxamates show toxicity at higher concentrations. Our present results appear to be consistent with the possibility that the mercaptoacetamide-based HDAC inhibitors interact with a different subset of the HDAC isozymes [less activity at HDAC1 and 2 correlates with less inhibitor toxicity], or alternatively, are interacting selectively with only the cytoplasmic HDACs that are crucial for protection from oxidative stress.
Chemistry and biology of mercaptoacetamides as novel histone deacetylase inhibitors
Chen, Bin,Petukhov, Pavel A.,Jung, Mira,Velena, Alfredo,Eliseeva, Elena,Dritschilo, Anatoly,Kozikowski, Alan P.
, p. 1389 - 1392 (2007/10/03)
A series of mercaptoacetamides were designed and synthesized as novel histone deacetylase inhibitors with the aid of modeling. Their ability to inhibit HDAC activity and their effects on cancer cell growth were investigated. Some compounds exhibit better
