- Title
- Expansion of a Synthesized Library of N-Benzyl Sulfonamides Derived from an Indole Core to Target Pancreatic Cancer
- Creator
- Hopkins, Megan D.; Costello, Ian J.; Chiew, Beatrice; McCluskey, Adam; Sheaff, Robert J.; Lamar, Angus A.; Brandeburg, Zachary C.; Slay, Emily L.; Zanders, Levi A.; Dunn, Caroline E.; Derewonko, Carina A.; Davitt, Colin L.; Reeder, Madison A.; Prichard, Kate
- Relation
- ChemMedChem Vol. 18, Issue 19, no. e202300265
- Publisher Link
- http://dx.doi.org/10.1002/cmdc.202300265
- Publisher
- Wiley-VCH Verlag GmbH & Co. KGaA
- Resource Type
- journal article
- Date
- 2023
- Description
- In an effort to further investigate previously observed activity of indolyl sulfonamides towards pancreatic cancer cell lines, a library of 44 compounds has been synthesized. The biological activity of the compounds has been determined using two different screening assay techniques against 7 pancreatic cancer cell lines and 9 non-pancreatic cancer cell lines. In the first assay, the cytotoxicity of the compounds was evaluated using a traditional (48 hour compound exposure) method. An in silico investigation was conducted to determine if the compounds might be inducing cell death by inhibiting the S100A2-p53 protein-protein interaction. In the second assay, the potential role of the compounds as metabolic inhibitors of ATP production was evaluated using a rapid screening (1–2 hour compound exposure) method. IC50 values of the hit compounds were obtained and four compounds displayed sub-micromolar potency against PANC-1 cells. The investigation has provided several compounds that display selective in vitro activity toward pancreatic cancer that warrant further development.
- Subject
- 2-deoxy-D-glucose; indole; metabolic inhibitors; pancreatic cancer; sulfonamides; SDG 3; Sustainable Development Goals
- Identifier
- http://hdl.handle.net/1959.13/1494372
- Identifier
- uon:53783
- Identifier
- ISSN:1860-7179
- Language
- eng
- Hits: 2191
- Visitors: 2117
- Downloads: 0
| Thumbnail | File | Description | Size | Format |
|---|