Synthesis and screening of 3-substituted thioxanthen-9-one-10,10-dioxides.
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.
Lory
Pedro M J
PM
Department of Pharmacology and Toxicology,Chemical Biology Program, University of Texas Medical Branch, 301 University Boulevard, Galveston, TX 77555-0650, USA.
Estrella-Jimenez
Maria E
ME
Shashack
Matthew J
MJ
Lokesh
Ganesh L
GL
Natarajan
Amarnath
A
Gilbertson
Scott R
SR
D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D005454:Fluorescence Polarization; D016174:Hepacivirus / Q000187:drug effects; D014966:Xanthenes / Q000138:chemical synthesis* / Q000494:pharmacology*