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. 2018 Oct 23;9:4399. doi: 10.1038/s41467-018-06703-2

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© The Author(s) 2018

Open Access This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The images or other third party material in this article are included in the article’s Creative Commons license, unless indicated otherwise in a credit line to the material. If material is not included in the article’s Creative Commons license and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this license, visit http://creativecommons.org/licenses/by/4.0/.

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Fig. 1 — Chemical progression of pantazines. a Lipophilic ligand efficiency (LipE = pIC₅₀ – clogP) guided optimization of the pantazine series from the initial hit (PZ-2789) to PZ-2891. b Summary of the structure-activity relationships of >60 compounds synthesized during the optimization of the pantazine scaffold. c Chemical structure of an inactive pantazine, PZ-3067, which is used as a negative control in cellular assays