5535-03-5Relevant articles and documents
Nonpeptidic propargylamines as inhibitors of lysine specific demethylase 1 (LSD1) with cellular activity
Schmitt, Martin L.,Hauser, Alexander-Thomas,Carlino, Luca,Pippel, Martin,Schulz-Fincke, Johannes,Metzger, Eric,Willmann, Dominica,Yiu, Teresa,Barton, Michelle,Schüle, Roland,Sippl, Wolfgang,Jung, Manfred
supporting information, p. 7334 - 7342 (2013/10/21)
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 LSD1 containing a propargylamine warhead, starting out from lysine containing substrate analogues. On the basis of these substrate mimicking inhibitors, we were able to increase potency by a combination of similarity-based virtual screening and subsequent synthetic optimization resulting in more druglike LSD1 inhibitors that led to histone hypermethylation in breast cancer cells.
SYNTHESIS AND PHARMACOLOGICAL ACTIVITY OF SOME 1-PHENOXY-3-AMINO-PROPAN-2-OLS
Glozman, O. M.,Orlova, E. K.,Zhmurenko, L. A.,Meshcheryakova, L. M.,Kuznetsova, G. A.,et al.
, p. 469 - 473 (2007/10/02)
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Ultra-Short-Acting β-Adrenergic Receptor Blocking Agents. 2. (Aryloxy)propanolamines Containing Esters on the Aryl Function
Erhardt, Paul W.,Woo, Chi M.,Anderson, William G.,Gorczynski, Richard J.
, p. 1408 - 1412 (2007/10/02)
Several short-acting β-adrenergic receptor blocking agents have been prepared by incorporating ester functions into the aryl portion of certain (aryloxy)propanolamine systems.In particular, methyl 3-phenyl>propionate hydrochloride (ASL-8052) was found to be a moderately potent, cardioselective compound with a short duration of action when determined in in vivo canine models.