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Discovery of Novel Cinchona‐Alkaloid‐Inspired Oxazatwistane Autophagy Inhibitors
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2017 (English)In: Angewandte Chemie International Edition, ISSN 1433-7851, E-ISSN 1521-3773, Vol. 56, no 8, p. 2145-2150Article in journal (Refereed) Published
Abstract [en]

The cinchona alkaloids are a privileged class of natural products and are endowed with diverse bioactivities. However, for compounds with the closely‐related oxazatricyclo[4.4.0.0]decane (“oxazatwistane”) scaffold, which are accessible from cinchonidine and quinidine by means of ring distortion and modification, biological activity has not been identified. We report the synthesis of an oxazatwistane compound collection through employing state‐of‐the‐art C−H functionalization, and metal‐catalyzed cross‐coupling reactions as key late diversity‐generating steps. Exploration of oxazatwistane bioactivity in phenotypic assays monitoring different cellular processes revealed a novel class of autophagy inhibitors termed oxautins, which, in contrast to the guiding natural products, selectively inhibit autophagy by inhibiting both autophagosome biogenesis and autophagosome maturation.

Place, publisher, year, edition, pages
2017. Vol. 56, no 8, p. 2145-2150
National Category
Organic Chemistry
Research subject
computational linguistics
Identifiers
URN: urn:nbn:se:umu:diva-157488DOI: 10.1002/anie.201611670OAI: oai:DiVA.org:umu-157488DiVA, id: diva2:1299169
Funder
EU, European Research Council, 678899Available from: 2019-03-26 Created: 2019-03-26 Last updated: 2019-03-28Bibliographically approved

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Wu, Yao-Wen

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