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Divergent synthesis of a thiolate-based α-hydroxytropolone library with a dynamic bioactivity profile.


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, and a human hepatoblastoma (HepDES19) revealed complementary biological profiles and new lead compounds with sub-micromolar activity against each pathogen.

SUBMITTER: Agyemang NB 

PROVIDER: S-EPMC7543996 | biostudies-literature | 2019

REPOSITORIES: biostudies-literature