Max Planck Institute of Molecular Physiology , Otto-Hahn-Straße 11, 44227 Dortmund, Germany.
Faculty of Chemistry and Chemical Biology, Technical University Dortmund , Otto-Hahn-Straßa 6, 44221 Dortmund, Germany.
J Org Chem. 2016 Nov 4;81(21):10242-10255. doi: 10.1021/acs.joc.6b01185. Epub 2016 Jul 15.
Iridoids comprise a large group of monoterpenoid natural products displaying a diverse array of biological activities ranging from neurotrophic to anti-inflammatory and anti-tumorigenic properties. Therefore, the development of concise synthesis routes to compound collections inspired by the structural features of these natural products is of particular relevance for chemical biology and medicinal chemistry. Herein we describe a samarium diiodide-mediated synthesis of a small, focused iridoid-inspired compound collection. Characterization of these iridoid analogues in biological assays revealed novel small-molecule inhibitors of autophagy.
环烯醚萜类化合物是一大类单萜类天然产物，具有多种多样的生物活性，包括神经营养、抗炎和抗肿瘤特性。因此，开发受这些天然产物结构特征启发的化合物库的简洁合成途径对于化学生物学和药物化学具有特别重要的意义。在此，我们描述了一种基于钐二碘化物介导的方法合成的小而集中的环烯醚萜类化合物库。这些环烯醚萜类似物在生物测定中的特征分析揭示了新型的自噬小分子抑制剂。
