1259287-72-3Relevant academic research and scientific papers
Potent histone deacetylase inhibitors derived from 4-(aminomethyl)-N- hydroxybenzamide with high selectivity for the HDAC6 isoform
Blackburn, Christopher,Barrett, Cynthia,Chin, Janice,Garcia, Kris,Gigstad, Kenneth,Gould, Alexandra,Gutierrez, Juan,Harrison, Sean,Hoar, Kara,Lynch, Chrissie,Rowland, R. Scott,Tsu, Chris,Ringeling, John,Xu, He
, p. 7201 - 7211 (2013/10/21)
A screen for HDAC6 inhibitors identified acyl derivatives of 4-(aminomethyl)-N-hydroxybenzamide as potent leads with unexpected selectivity over the other subtypes. We designed and synthesized constrained heterocyclic analogues such as tetrahydroisoquinolines that show further enhanced HDAC6 selectivity and inhibitory activity in cellular assays. Selectivity may be attributed to the benzylic spacer more effectively accessing the wider channel of HDAC6 compared to other HDAC subtypes as well as hydrophobic capping groups interacting with the protein surface near the rim of the active site.
SUBSTITUTED HYDROXAMIC ACIDS AND USES THEREOF
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Page/Page column 98; 99; 100, (2011/01/12)
This invention provides compounds of formula (/): wherein R1, R2, G, n, p and q have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the comp
