Nonpeptidic propargylamines as inhibitors of lysine specific demethylase 1 (LSD1) with cellular activity

…, J Schulz-Fincke, E Metzger, D Willmann…

Index: Schmitt, Martin L.; Hauser, Alexander-Thomas; Carlino, Luca; Pippel, Martin; Schulz-Fincke, Johannes; Metzger, Eric; Willmann, Dominica; Yiu, Teresa; Barton, Michelle; Schuele, Roland; Sippl, Wolfgang; Jung, Manfred Journal of Medicinal Chemistry, 2013 , vol. 56, # 18 p. 7334 - 7342

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Citation Number: 20

Abstract

Lysine demethylases play an important role in epigenetic regulation and thus in the development of diseases like cancer or neurodegenerative disorders. As the lysine specific demethylase 1 (LSD1/KDM1) has been strongly connected to androgen and estrogen dependent gene expression, it serves as a promising target for the therapy of hormone dependent cancer. Here, we report on the discovery of new small molecule inhibitors of ...