900176-67-2Relevant academic research and scientific papers
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 DERIVATIVES
-
Page/Page column 38, (2008/06/13)
The invention concerns benzamide compounds of Formula (I) wherein W, R, X , and Q are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and the
N-PHENYL-4-PYRIDIN-2-YL-BENZAMIDE DERIVATIVES AS HISTONE DEACYLASE (HDAC) INHIBITORS FOR THE TREATMENT OF CANCER
-
Page/Page column 92, (2008/06/13)
The invention concerns benzamide derivatives of Formula (I) wherein R1a, R1b, R1c, R2, R3, R4, W, m and n have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours or other proliferative conditions which are sensitive to the inhibition of histone deacetylase (HDAC).
