1314323-95-9Relevant academic research and scientific papers
KDM1A INHIBITORS FOR THE TREATMENT OF DISEASE
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, (2016/09/26)
Disclosed herein are new compounds and compositions and their application as pharmaceuticals for the treatment of diseases. Methods of inhibition of KDMIA, methods of increasing gamma globin gene expression, and methods to induce differentiation of cancer cells in a human or animal subject are also provided for the treatment of diseases such as acute myelogenous leukemia.
Enantioselective synthesis of tranylcypromine analogues as lysine demethylase (LSD1) inhibitors
Benelkebir, Hanae,Hodgkinson, Christopher,Duriez, Patrick J.,Hayden, Annette L.,Bulleid, Rosemary A.,Crabb, Simon J.,Packham, Graham,Ganesan
, p. 3709 - 3716 (2011/08/02)
Asymmetric cyclopropanation of styrenes by tert-butyl diazoacetate followed by ester hydrolysis and Curtius rearrangement gave a series of tranylcypromine analogues as single enantiomers. The o,- m- and p-bromo analogues were all more active than tranylcypromine in a LSD1 enzyme assay. The m- and p-bromo analogues were micromolar growth inhibitors of the LNCaP prostate cancer cell line as were the corresponding biphenyl analogues prepared from the bromide by Suzuki crosscoupling.
