structure–activity relationships and biological evaluation of 7-substituted harmine analogs for human β-cell proliferation

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ID: 136593
2020
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Abstract
Recently, we have shown that harmine induces β-cell proliferation both in vitro and in vivo, mediated via the DYRK1A-NFAT pathway. We explore structure–activity relationships of the 7-position of harmine for both DYRK1A kinase inhibition and β-cell proliferation based on our related previous structure–activity relationship studies of harmine in the context of diabetes and β-cell specific targeting strategies. 33 harmine analogs of the 7-position substituent were synthesized and evaluated for biological activity. Two novel inhibitors were identified which showed DYRK1A inhibition and human β-cell proliferation capability. The DYRK1A inhibitor, compound 1-2b, induced β-cell proliferation half that of harmine at three times higher concentration. From these studies we can draw the inference that 7-position modification is limited for further harmine optimization focused on β-cell proliferation and cell-specific targeting approach for diabetes therapeutics.
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kumar2020moleculesstructureactivity Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Kunal Kumar, Peng Wang, Ethan A. Swartz, Susmita Khamrui, Cody Secor, Michael B. Lazarus, Roberto Sanchez, Andrew F. Stewart, Robert J. DeVita
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Journal Journal of ethnopharmacology
Year 2020
DOI
10.3390/molecules25081983
URL
https://www.mdpi.com/1420-3049/25/8/1983
Keywords Keywords not found

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