1314867-11-2Relevant academic research and scientific papers
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.
5-HT2C RECEPTOR AGONISTS AS ANORECTIC AGENTS
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Page/Page column 130, (2008/06/13)
This invention relates to compounds which modulate receptors of the 5-HT2 family of receptors, and particularly to compounds which modulate 5-HT2C receptors. Compounds of the invention include agonists and selective agonists for the 5-HT2C receptor. Compounds of the invention include selective agonists for the 5-HT2C receptor which exhibit significantly less or no agonist activity on the 5-HT2A receptor and/or the 5-HT2B receptor. Compounds of this invention are those of Formula I and pharmaceutically acceptable salts, esters and solvates (including hydrates) wherein variables are defined in the specification hereof.
