151707-53-8Relevant articles and documents
New small molecule inhibitors of histone methyl transferase DOT1L with a nitrile as a non-traditional replacement for heavy halogen atoms
Spurr, Sophie S.,Bayle, Elliott D.,Yu, Wenyu,Li, Fengling,Tempel, Wolfram,Vedadi, Masoud,Schapira, Matthieu,Fish, Paul V.
, p. 4518 - 4522 (2016/08/24)
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.
Synthesis and evaluation of Janus type nucleosides as potential HCV NS5B polymerase inhibitors
Zhou, Longhu,Amblard, Franck,Zhang, Hongwang,McBrayer, Tamara R.,Detorio, Mervi A.,Whitaker, Tony,Coats, Steven J.,Schinazi, Raymond F.
, p. 3385 - 3388 (2013/06/27)
The synthesis of new ribo and 2′-β-C-methyl ribo Janus type nucleosides J-AA, J-AG and J-AU is reported along with their ability to block HCV and HIV replication. Their toxicity was also assessed in Huh7, human lymphocytes, CEM and Vero cells.
Total synthesis of the naturally occurring antibiotic toyocamycin using new and improved synthetic procedures
Porcari, Anthony R.,Townsend, Leroy B.
, p. 153 - 159 (2007/10/03)
Starting with commercially available tetracyanoethylene, we describe a more efficient and higher yielding synthesis of toyocamycin with regards to convenience, overall yield, and total reaction time than those syntheses previously reported.