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Synthesis and screening of 3-substituted thioxanthen-9-one-10,10-dioxides.

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.

SUBMITTER: Lory PM 

PROVIDER: S-EPMC2040121 | biostudies-literature | 2007 Nov

REPOSITORIES: biostudies-literature

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Synthesis and screening of 3-substituted thioxanthen-9-one-10,10-dioxides.

Lory Pedro M J PM   Estrella-Jimenez Maria E ME   Shashack Matthew J MJ   Lokesh Ganesh L GL   Natarajan Amarnath A   Gilbertson Scott R SR  

Bioorganic & medicinal chemistry letters 20070825 21

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 alk  ...[more]

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