Novel tertiary sulfonamides as potent anti-cancer agents.
Autor: | Okolotowicz KJ; Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, CA 92121, USA., Dwyer M; Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, CA 92121, USA., Ryan D; Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, CA 92121, USA., Cheng J; Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, CA 92121, USA., Cashman EA; Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, CA 92121, USA., Moore S; Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, CA 92121, USA., Mercola M; Cardiovascular Institute and Department of Medicine, Stanford University, 300 Pasteur Dr., MC-5501, Stanford, CA 94305, USA., Cashman JR; Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, CA 92121, USA. Electronic address: JCashman@HBRI.org. |
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Jazyk: | angličtina |
Zdroj: | Bioorganic & medicinal chemistry [Bioorg Med Chem] 2018 Aug 15; Vol. 26 (15), pp. 4441-4451. Date of Electronic Publication: 2018 Jul 25. |
DOI: | 10.1016/j.bmc.2018.07.042 |
Abstrakt: | For adult women in the United States, breast cancer is the most prevalent form of cancer. Compounds that target dysregulated signal transduction can be efficacious anti-cancer therapies. A prominent signaling pathway frequently dysregulated in breast cancer cells is the Wingless-related integration site (Wnt) pathway. The purpose of the work was to optimize a "hit" from a screening campaign. 76,000 compounds were tested in a Wnt transcription assay and revealed potent and reproducible "hit," compound 1. Medicinal chemistry optimization of 1 led to more potent and drug-like molecules, 19, 24 and 25 (i.e., Wnt pathway IC (Copyright © 2018 Elsevier Ltd. All rights reserved.) |
Databáze: | MEDLINE |
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