Bioorganic and Medicinal Chemistry Letters p. 4518 - 4522 (2016)
Update date:2022-08-04
Topics:
Spurr, Sophie S.
Bayle, Elliott D.
Yu, Wenyu
Li, Fengling
Tempel, Wolfram
Vedadi, Masoud
Schapira, Matthieu
Fish, Paul V.
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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