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Updated: Dec 6, 2025

Synthesis and Bioconjugation of Thiol-Reactive Reagents for the Creation of Site-Selectively Modified Immunoconjugates
Published on: March 6, 2019
Divergent synthesis of a thiolate-based α-hydroxytropolone library with a dynamic bioactivity profile
Nana B Agyemang1,2, Cassandra R Kukla3, Tiffany C Edwards3
1Department of Chemistry, Brooklyn College, The City University of New York, Brooklyn, New York 11210, United States.
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.
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