1030927-09-3Relevant articles and documents
Flexible and scalable route to HDAc inhibitors containing an unusual trisubstituted pyridine core
Graham, Mark A.,Raw, Steven A.,Andrews, David M.,Good, Catherine J.,Matusiak, Zbigniew S.,Maybury, Mark,Stokes, Elaine S. E.,Turner, Andrew T.
, p. 1283 - 1292 (2012)
A scalable route to histone deacetylase inhibitors containing an unusual 2-aryl-3-cyano-5-aminomethylpyridine core has been developed which has the flexibility to deliver a range of compounds on at least a multigram scale. The key step involves a novel Ma
Design and campaign synthesis of pyridine-based histone deacetylase inhibitors
Andrews, David M.,Gibson, Keith M.,Graham, Mark A.,Matusiak, Zbigniew S.,Roberts, Craig A.,Stokes, Elaine S.E.,Brady, Madeleine C.,Chresta, Christine M.
, p. 2525 - 2529 (2008/12/21)
A lead benzamide, bearing a cyanopyridyl moiety (3), was identified as a potent and low molecular weight histone deacetylase (HDAC) inhibitor. Various replacements of the cyano group were explored at the C3-position, along with the exploration of solubility-enhancing groups at the C5-position. It was determined that cyano substitution at the C3-position of the pyridyl core, along with a methylazetidinyl substituent at the C5-position yielded optimal HDAC1 inhibition and anti-proliferative activity in HCT-116 cells.
Benzamide Compounds
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Page/Page column 63, (2009/01/20)
The invention concerns benzamide compounds of Formula (I), wherein R1a, R1b, R1c, R2, R3, R4, m and n have any of the meanings defined in the description; processes for their preparation, p
