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Issue 59, 2019
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Divergent synthesis of a thiolate-based α-hydroxytropolone library with a dynamic bioactivity profile

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Abstract

Here we describe a rapid and divergent synthetic route toward structurally novel αHTs functionalized with either one or two thioether or sulfonyl appendages. Evaluation of this library against hepatitis B and herpes simplex virus, as well as the pathogenic fungus Cryptococcus neoformans, revealed complementary biological profiles and new lead compounds with sub-micromolar activities against each pathogen and high selectivities when compared to mammalian cell lines.

Graphical abstract: Divergent synthesis of a thiolate-based α-hydroxytropolone library with a dynamic bioactivity profile

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Publication details

The article was received on 15 Aug 2019, accepted on 07 Oct 2019 and first published on 23 Oct 2019


Article type: Paper
DOI: 10.1039/C9RA06383H
RSC Adv., 2019,9, 34227-34234
  • Open access: Creative Commons BY-NC license
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    Divergent synthesis of a thiolate-based α-hydroxytropolone library with a dynamic bioactivity profile

    N. B. Agyemang, C. R. Kukla, T. C. Edwards, Q. Li, M. K. Langen, A. Schaal, A. D. Franson, A. G. Casals, K. A. Donald, A. J. Yu, M. J. Donlin, L. A. Morrison, J. E. Tavis and R. P. Murelli, RSC Adv., 2019, 9, 34227
    DOI: 10.1039/C9RA06383H

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