Amphipathic alpha-Helix Mimetics Based on a 1,2-Diphenylacetylene Scaffold

作者:Jung Kwan Young; Vanommeslaeghe Kenno; Lanning Maryanna E; Yap Jeremy L; Gordon Caryn; Wilder Paul T; MacKerell Alexander D Jr; Fletcher Steven*
来源:Organic Letters, 2013, 15(13): 3234-3237.
DOI:10.1021/ol401197n

摘要

In order to mimic amphipathic alpha-helices, a novel scaffold based on a 1,2-diphenylacetylene was designed. NMR and computational modeling confirmed that an intramolecular hydrogen bond favors conformations of the 1,2-diphenylacetylene that allow for accurate mimicry of the i, i + 7 and i + 2, i + 5 side chains found on opposing faces of an alpha-helix.

  • 出版日期2013-7-5