Open Access. Powered by Scholars. Published by Universities.®
- Publication
- Publication Type
Articles 1 - 3 of 3
Full-Text Articles in Molecular Biology
Cell Proliferation And Viability Inhibition By Resveratrol On Breast Cancer Cell Lines, Kyle Ford Gordon Jr
Cell Proliferation And Viability Inhibition By Resveratrol On Breast Cancer Cell Lines, Kyle Ford Gordon Jr
Honors Theses
Antioxidants are well-known for their various health benefits. They are able to protect cells from being damaged by free radicals that are produced by vital biochemical processes. It has long been known that antioxidants are important in our everyday health, but their potential as disease preventers and potential therapeutic agents is a relatively new field of study. Resveratrol, a natural polyphenol and well-known antioxidant, is found in plants, fruits, and products derived from them, like red wine. Resveratrol has been shown to have various properties, including antiaging, anti-aggregation of platelets, anti-inflammatory, and anticancer activities. Because of their many health benefits, …
The Effects Of Largazole, A Histone Deacetylase Inhibitor, On Breast Cancer Cell Viability And Metastasis, Hannah Mccowan
The Effects Of Largazole, A Histone Deacetylase Inhibitor, On Breast Cancer Cell Viability And Metastasis, Hannah Mccowan
Honors Theses
Histone deacetylase enzymes modify epigenetic characteristics of a genome by removing acetyl groups from histone proteins in chromatin. Histone deacetylase inhibitors work by stopping this activity which can have various results in a cell including apoptosis, cell cycle arrest, differentiation, and migration. The purpose of these experiments was to see how largazole, a histone deacetylase inhibitor, affected cell viability for breast cancer and associated metastatic cell lines in both normoxic and hypoxic conditions. The experiment was completed by setting up two 96-well plates with varying concentrations of largazole and conducting a sulforhodamine viability assay. The specific cell lines used in …
Optimisation Of Estrogen Receptor Subtype-Selectivity Of A 4-Aryl-4h-Chromene Scaffold Previously Identified By Virtual Screening, Miriam Carr, Andrew Knox, Daniel Nevin, Niamh O'Boyle, Shu Wang, Billy Egan, Thomas Mccabe, Brendan Twamley, Daniela Zisterer, David Lloyd, Mary Meegan
Optimisation Of Estrogen Receptor Subtype-Selectivity Of A 4-Aryl-4h-Chromene Scaffold Previously Identified By Virtual Screening, Miriam Carr, Andrew Knox, Daniel Nevin, Niamh O'Boyle, Shu Wang, Billy Egan, Thomas Mccabe, Brendan Twamley, Daniela Zisterer, David Lloyd, Mary Meegan
Articles
4-Aryl-4H-Chromene derivatives have been previously shown to exhibit anti-proliferative, apoptotic and anti-angiogenic activity in a variety of tumor models in vitro and in vivo generally via activation of caspases through inhibition of tubulin polymerisation. We have previously identified by Virtual Screening (VS) a 4-aryl-4H-chromene scaffold, of which two examples were shown to bind Estrogen Receptor α and β with low nanomolar affinity and <20-fold selectivity for α over β and low micromolar anti-proliferative activity in the MCF-7 cell line. Thus, using the 4-aryl-4H-chromene scaffold as a starting point, a series of compounds with a range of basic arylethers at C-4 and modifications at the C3-ester substituent of the benzopyran ring were synthesised, producing some potent ER antagonists in the MCF-7 cell line which were highly selective for ERα (compound 35; 350-fold selectivity) or ERβ (compound 42; 170-fold selectivity).