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Publication Detail
New small molecule inhibitors of histone methyl transferase DOT1L with a nitrile as a non-traditional replacement for heavy halogen atoms.
  • Publication Type:
    Journal article
  • Publication Sub Type:
  • Authors:
    Spurr SS, Bayle ED, Yu W, Li F, Tempel W, Vedadi M, Schapira M, Fish PV
  • Publication date:
  • Journal:
    Bioorganic & medicinal chemistry letters
  • Medium:
  • Print ISSN:
  • Language:
  • Addresses:
    UCL School of Pharmacy, University College London, 29-39 Brunswick Square, London WC1N 1AX, UK.
A number of new nucleoside derivatives are disclosed as inhibitors of DOT1L activity. SARs established that DOT1L inhibition could be achieved through incorporation of polar groups and small heterocycles at the 5-position (5, 6, 12) or by the application of alternative nitrogenous bases (18). Based on these results, CN-SAH (19) was identified as a potent and selective inhibitor of DOT1L activity where the polar 5-nitrile group was shown by crystallography to bind in the hydrophobic pocket of DOT1L. In addition, we show that a polar nitrile group can be used as a non-traditional replacement for heavy halogen atoms.
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