کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1361225 981459 2011 8 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Enantioselective synthesis of tranylcypromine analogues as lysine demethylase (LSD1) inhibitors
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Enantioselective synthesis of tranylcypromine analogues as lysine demethylase (LSD1) inhibitors
چکیده انگلیسی

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.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 19, Issue 12, 15 June 2011, Pages 3709–3716
نویسندگان
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