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Synthesis and Bioconjugation of Thiol-Reactive Reagents for the Creation of Site-Selectively Modified Immunoconjugates
Published on: March 6, 2019
Synthesis and screening of 3-substituted thioxanthen-9-one-10,10-dioxides
Pedro M J Lory1, Maria E Estrella-Jimenez, Matthew J Shashack
1Department of Pharmacology and Toxicology,Chemical Biology Program, University of Texas Medical Branch, 301 University Boulevard, Galveston, TX 77555-0650, USA.
Abstract:
This manuscript describes methods appropriate for the parallel synthesis of libraries based on the tricyclic thioxanthen-9-one-10,10-dioxide scaffold. The novel compounds were synthesized from previously reported 3-chlorothioxanthen-9-one-10,10-dioxide and commercially available 3-carboxylic acid thioxanthen-9-one-10,10-dioxide. The library members were screened for activity in a fluorescence polarization assay for inhibitors of BRCT domains of breast cancer gene 1 and in cell-based secreted alkaline phosphatase reported replicon system for activity against hepatitis C virus.
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