structure–activity relationships and biological evaluation of 7-substituted harmine analogs for human β-cell proliferation
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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.
| Reference Key |
kumar2020moleculesstructureactivity
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|---|---|
| Authors | ;Kunal Kumar;Peng Wang;Ethan A. Swartz;Susmita Khamrui;Cody Secor;Michael B. Lazarus;Roberto Sanchez;Andrew F. Stewart;Robert J. DeVita |
| Journal | Journal of ethnopharmacology |
| Year | 2020 |
| DOI |
10.3390/molecules25081983
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| URL | |
| Keywords | Keywords not found |
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