934828-17-8Relevant academic research and scientific papers
Design and campaign synthesis of piperidine- and thiazole-based histone deacetylase inhibitors
Andrews, David M.,Stokes, Elaine S.E.,Carr, Greg R.,Matusiak, Zbigniew S.,Roberts, Craig A.,Waring, Michael J.,Brady, Madeleine C.,Chresta, Christine M.,East, Simon J.
, p. 2580 - 2584 (2008/12/21)
A lead benzamide, 3, was identified as a potent and low molecular weight histone deacetylase (HDAC) inhibitor. Optimization led to 16d, demonstrating an excellent balance of efficacy and non-efficacy properties, along with very desirable in vivo DMPK. The
BENZAMIDE COMPOUNDS USEFUL AS HISTONE DEACETYLASE INHIBITORS
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Page/Page column 46, (2010/11/27)
The invention concerns benzamide compounds of formula (I), wherein R1 is a C-linked pyrazole ring, which is optionally substituted by one or more groups selected from C1-4alkyl, C3-4cycloalkyl, C1-4alkoxy and C3-4 cycloalkoxy; or a pharmaceutically acceptable salt or pro-drug form thereof. The invention also concerns processes for the preparation of such compounds, 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).
