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  • Title: Design and campaign synthesis of pyridine-based histone deacetylase inhibitors.
    Author: Andrews DM, Gibson KM, Graham MA, Matusiak ZS, Roberts CA, Stokes ES, Brady MC, Chresta CM.
    Journal: Bioorg Med Chem Lett; 2008 Apr 15; 18(8):2525-9. PubMed ID: 18378451.
    Abstract:
    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.
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